List Of Opioids
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opioid Opioids are substances that act on opioid receptors to produce morphine-like effects. Medically they are primarily used for pain relief, including anesthesia. Other medical uses include suppression of diarrhea, replacement therapy for opioid us ...
s,
opioid antagonist An opioid antagonist, or opioid receptor antagonist, is a receptor antagonist that acts on one or more of the opioid receptors. Naloxone and naltrexone are commonly used opioid antagonist drugs which are competitive antagonists that bind to the o ...
s and
inverse agonist In pharmacology, an inverse agonist is a drug that binds to the same receptor as an agonist but induces a pharmacological response opposite to that of the agonist. A neutral antagonist has no activity in the absence of an agonist or inverse agon ...
s.


Opium Opium (or poppy tears, scientific name: ''Lachryma papaveris'') is dried latex obtained from the seed capsules of the opium poppy ''Papaver somniferum''. Approximately 12 percent of opium is made up of the analgesic alkaloid morphine, which i ...
and
poppy straw Poppy straw (also known as opium straw, mowed opium straw, crushed poppy capsule, poppy chaff, or poppy husk) is derived from opium poppies (''Papaver somniferum'') that are harvested when fully mature and dried by mechanical means, minus the rip ...
derivatives


Crude opiate extracts whole opium products

* B&O Supprettes * Diascordium *
Dover's powder Dover's powder was a traditional medicine against cold and fever developed by Thomas Dover. It is no longer in use in modern medicine, but may have been in use at least through the 1960s. A 1958 source describes Dover's Powder as follows: "Powder ...
*
Kendal Black Drop Kendal Black Drop was a drug based on opium. Named after Kendal on the edge of the Lake District, England, it is associated with the romantic poet, Samuel Taylor Coleridge. Description Black Drop was a 19th-century dark medicine made of opium, vin ...
*
Laudanum Laudanum is a tincture of opium containing approximately 10% powdered opium by weight (the equivalent of 1% morphine). Laudanum is prepared by dissolving extracts from the opium poppy (''Papaver somniferum Linnaeus'') in alcohol (ethanol). Red ...
*
Mithridate Mithridate, also known as mithridatium, mithridatum, or mithridaticum, is a semi-mythical remedy with as many as 65 ingredients, used as an antidote for poisoning, and said to have been created by Mithridates VI Eupator of Pontus in the 1st cent ...
*
Opium Opium (or poppy tears, scientific name: ''Lachryma papaveris'') is dried latex obtained from the seed capsules of the opium poppy ''Papaver somniferum''. Approximately 12 percent of opium is made up of the analgesic alkaloid morphine, which i ...
*
Polish heroin "Polish" heroin (also ''kompot'' and compote in drug culture slang) is a crude preparation of heroin made from poppy straw. It is an opiate, used recreationally as a psychoactive drug. Poppy straw, like opium, is harvested from the opium poppy ...
 (Compote, Kompot) *
Paregoric Paregoric, or camphorated tincture of opium, also known as ''tinctura opii camphorata'', is a traditional patent medicine known for its antidiarrheal, antitussive, and analgesic properties. According to Goodman and Gilman's 1965 edition, "Par ...
*
Poppy straw concentrate Poppy straw (also known as opium straw, mowed opium straw, crushed poppy capsule, poppy chaff, or poppy husk) is derived from opium poppies (''Papaver somniferum'') that are harvested when fully mature and dried by mechanical means, minus the ri ...
*
Poppy tea Poppy tea is an herbal tea infusion brewed from poppy straw or seeds of several species of poppy. The species most commonly used for this purpose is ''Papaver somniferum'', which produces opium as a natural defense against predators. In the liv ...
* Smoking opium *
Theriac Theriac or theriaca is a medical concoction originally labelled by the Greeks in the 1st century AD and widely adopted in the ancient world as far away as Persia, China and India via the trading links of the Silk Route. It was an alexipharmic, ...


Natural opiates


Opium alkaloids

*
Codeine Codeine is an opiate and prodrug of morphine mainly used to treat pain, coughing, and diarrhea. It is also commonly used as a recreational drug. It is found naturally in the sap of the opium poppy, ''Papaver somniferum''. It is typically use ...
*
Morphine Morphine is a strong opiate that is found naturally in opium, a dark brown resin in poppies (''Papaver somniferum''). It is mainly used as a analgesic, pain medication, and is also commonly used recreational drug, recreationally, or to make ...
*
Oripavine Oripavine is an opioid and the major metabolite of thebaine. It is the parent compound from which a series of semi-synthetic opioids are derived, which includes the compounds etorphine and buprenorphine. Although its analgesic potency is compar ...
*
Pseudomorphine Pseudomorphine (also known as oxydimorphine or dehydromorphine) is an inactive, natural dimerisation product of the morphine molecule in tandem and thus a common impurity in morphine concentrations. It was first described by Pelletier in 1835. ...
*
Thebaine Thebaine (paramorphine), also known as codeine methyl enol ether, is an opiate alkaloid, its name coming from the Greek Θῆβαι, '' Thēbai'' (Thebes), an ancient city in Upper Egypt. A minor constituent of opium, thebaine is chemically similar ...


Alkaloid salts mixtures

*
Pantopon Pantopon, also known as Opium Alkaloids Hydrochlorides, is a preparation of opiates made up of all of the alkaloids present in opium in their natural proportions as hydrochlorides salts. It can sometimes be tolerated by people who are allergic to ...
*
Papaveretum Papaveretum (BAN) is a preparation containing a mixture of hydrochloride salts of opium alkaloids. Since 1993, papaveretum has been defined in the British Pharmacopoeia (BP) as a mixture of 253 parts morphine hydrochloride, 23 parts papaverine hy ...
 (Omnopon) * Tetrapon


Semisynthetics including

Bentley compounds The Bentley compounds are a class of semi-synthetic opioids that were first synthesized by K. W. Bentley by Diels-Alder reaction of thebaine with various dienophiles. The compounds are also known as thevinols, orvinols, or bridged oripavine der ...


Morphine family

* 14-Hydroxymorphine  * 2,4-Dinitrophenylmorphine * 6-Methyldihydromorphine  *
6-Methylenedihydrodesoxymorphine 6-Methylenedihydrodesoxymorphine (6-MDDM) is an opiate analogue structurally related to desomorphine that is a derivative of hydromorphone, where the 6- ketone group has been replaced by a methylene group. It has sedative and analgesic effects ...
* 6-Acetyldihydromorphine  * Azidomorphine *
Chlornaltrexamine Chlornaltrexamine is an irreversible mixed agonist–antagonist for μ-opioid receptors, which forms a covalent bond to the active site. It is 22 times more potent than morphine. Its alkylating group is a bis(chloroalkyl)amino-residue similar to ...
*
Chloroxymorphamine Chloroxymorphamine is an opioid and a derivative of oxymorphone which binds irreversibly as an agonist to the μ-opioid receptor. See also * Chlornaltrexamine * Naloxazone * Oxymorphazone Oxymorphazone is an opioid analgesic drug related to ...
  *
Desomorphine Desomorphine is a semi-synthetic opioid commercialized by Roche, with powerful, fast-acting effects, such as sedation and analgesia. It was first discovered and patented by a German team working for Knoll in 1920 but was not generally recognized ...
 (dihydrodesoxymorphine) *
Dihydromorphine Dihydromorphine (Paramorfan, Paramorphan) is a semi-synthetic opioid structurally related to and derived from morphine. The 7,8-double bond in morphine is reduced to a single bond to get dihydromorphine.Rama Rao Nadendla. Principles Of Organic ...
* Ethyldihydromorphine chembase
cbid_346222 *
Hydromorphinol Hydromorphinol (RAM-320, 14-Hydroxydihydromorphine), also is an opiate analogue that is a derivative of morphine, where the 14-position has been hydroxylated and the 7,8- double bond saturated. It has similar effects to morphine such as sedation ...
* Methyldesorphine * Morphine methylbromide * N-Phenethylnordesomorphine *
N-Phenethyl-14-ethoxymetopon ''N''-Phenethyl-14-ethoxymetopon is a drug that is a derivative of metopon. It is a potent analgesic, around 60 times stronger than morphine and produces significantly less constipation. ''N''-Phenethyl-14-ethoxymetopon acts as an agonist at bo ...
*
N-Phenethylnormorphine ''N''-Phenethylnormorphine is an opioid analgesic drug derived from morphine by replacing the ''N''-methyl group with β-phenethyl. It is around eight to fourteen times more potent than morphine as a result of this modification, in contrast to m ...
* 6-Nicotinoyldihydromorphine (metabolite of
nicodicodeine Nicodicodine is an opioid developed as a cough suppressant and analgesic. Synthesized in 1904, it is not commonly used, but has activity similar to other opioids. Nicodicodine is metabolised in the liver by demethylation to produce 6-nicotinoyld ...
) *
RAM-378 RAM-378(7,8-Dihydro-14-hydroxy-N-phenethylnormorphine) is an opioid analgesic. It is the N-phenethyl derivative of hydromorphinol. See also * 14-Cinnamoyloxycodeinone * 14-Phenylpropoxymetopon * 7-PET * N-Phenethylnormorphine * N-Phenethyl-14-e ...
* Ro-1539


3,6-diesters of morphine

*
Acetylpropionylmorphine Acetylpropionylmorphine is an opiate analogue that is an ester of morphine. It was developed in the early 1900s after first being synthesised in Great Britain in 1875 but shelved along with heroin and various other esters of morphine. Acetylpropi ...
* 3,6-Dibutanoylmorphine * Diacetyldihydromorphine (dihydroheroin, acetylmorphinol) * Dibutyrylmorphine&nbs

*
Dibenzoylmorphine Dibenzoylmorphine is an opiate analogue that is a derivative of morphine. It was developed in the early 1900s after first having been synthesised in 1875 in the UK by the CR Alders Wright organisation at Bayer, along with various other esters of ...
 (first
designer drug A designer drug is a structural or functional analog of a controlled substance that has been designed to mimic the pharmacological effects of the original drug, while avoiding classification as illegal and/or detection in standard drug tests. Des ...
) * Diformylmorphine  *
Dipropanoylmorphine Dipropanoylmorphine (Dipropionylmorphine in U.S. English) is an opiate derivative, the 3,6-dipropanoyl ester of morphine. It was developed in 1972 as an analgesic. It is rarely used in some countries for the relief of severe pain such as that cause ...
*
Heroin Heroin, also known as diacetylmorphine and diamorphine among other names, is a potent opioid mainly used as a recreational drug for its euphoric effects. Medical grade diamorphine is used as a pure hydrochloride salt. Various white and brow ...
 (diacetylmorphine) *
Nicomorphine Nicomorphine (Vilan, Subellan, Gevilan, MorZet) is the 3,6-dinicotinate ester of morphine. It is a strong opioid agonist analgesic two to three times as potent as morphine with a side effect profile similar to that of dihydromorphine, morphine, a ...


Codeine-dionine family

* 6-Monoacetylcodeine *
Benzylmorphine Benzylmorphine (Peronine) is a semi-synthetic opioid narcotic introduced to the international market in 1896 and that of the United States very shortly thereafter. It is much like codeine, containing a benzyl group attached to the morphine molecu ...
* Codeine methylbromide * Desocodeine&nbs

* Dimethylmorphine (6-O-Methylcodeine)&nbs

* Ethyldihydromorphine&nbs

* Methyldihydromorphine (dihydroheterocodeine) *
Ethylmorphine Ethylmorphine (also known as codethyline, dionine, and ethyl morphine) is an opioid analgesic and antitussive. Side effects Adverse effects are similar to other opioids and include drowsiness, constipation, vertigo, nausea, vomiting, and respira ...
 (dionine) *
Heterocodeine Heterocodeine (6-methoxymorphine) is an opiate derivative, the 6-methyl ether of morphine, and a chemical structure, structural isomer of codeine; it is called "hetero-" because it is the reverse isomer of codeine. Heterocodeine was first synthes ...
* Isocodeine&nbs

*
Pholcodine Pholcodine is an opioid cough suppressant (antitussive). It helps suppress unproductive coughs and also has a mild sedative effect, but has little or no analgesic effects. It is also known as morpholinylethylmorphine and homocodeine. Pholcodine is ...
 (morpholinylethylmorphine) * Myrophine *
Thebacon Thebacon (INN; pronounced ), or dihydrocodeinone enol acetate, is a semisynthetic opioid that is similar to hydrocodone and is most commonly synthesised from thebaine. Thebacon was invented in Germany in 1924, four years after the first synthe ...
* Transisocodeine&nbs


Morphinones and morphols

*
14-Cinnamoyloxycodeinone 14-Cinnamoyloxycodeinone is the most potent example in a series of opiate analgesic drugs discovered in the 1960s, with > ×100 times the potency of morphine. It is a derivative of , being the 14-cinnamate ester. In another paper, Buckett assigns ...
* 14-Ethoxymetopon * 14-Methoxymetopon *
14-Phenylpropoxymetopon 14-Phenylpropoxymetopon (PPOM) is an opiate analogue that is a derivative of metopon which has been substituted with a γ-phenylpropoxy group at the 14-position. PPOM is a highly potent analgesic drug several thousand times stronger than morphine ...
* 3-Acetyloxymorphone * 3,14-Diacetyloxymorphone * 7-Spiroindanyloxymorphone * 8,14-Dihydroxydihydromorphinone&nbs

* Acetylcodone&nbs

* Acetylmorphone * α-hydrocodol  (=dihydrocodeine, ) * Benzhydrocodone * Bromoisopropropyldihydromorphinone cas? *
Codeinone Codeinone is 1/3 as active as codeine as an analgesic but it is an important intermediate in the production of hydrocodone, a painkiller about 3/4 the potency of morphine; as well as of oxycodone. The latter can also be synthesized from thebaine, ...
*
Codoxime Codoxime (Codossima) is an opiate analogue that is a derivative of hydrocodone, where the 6- ketone group has been replaced by carboxymethyloxime. It has primarily antitussive Cold medicines are a group of medications taken individually ...
* Conorfone (codorphone) * IBNtxA *
Thebacon Thebacon (INN; pronounced ), or dihydrocodeinone enol acetate, is a semisynthetic opioid that is similar to hydrocodone and is most commonly synthesised from thebaine. Thebacon was invented in Germany in 1924, four years after the first synthe ...
 (acetyldihydrocodeinone, dihydrocodeinone enol acetate) *
Hydrocodone Hydrocodone, also known as dihydrocodeinone, is an opioid used to treat pain and as a cough suppressant. It is taken by mouth. Typically it is dispensed as the combination acetaminophen/hydrocodone or ibuprofen/hydrocodone for pain severe en ...
*
Hydromorphone Hydromorphone, also known as dihydromorphinone, and sold under the brand name Dilaudid among others, is an opioid used to treat moderate to severe pain. Typically, long-term use is only recommended for pain due to cancer. It may be used by mou ...
* Hydroxycodeine&nbs

*
Metopon Metopon (5-methylhydromorphone) is an opioid analogue that is a methylated derivative of hydromorphone which was invented in 1929 as an analgesic. Metopon is sometimes used in medicine, although longer acting than hydromorphone, Metopon is less p ...
 (=methyldihydromorphinone) * Morphenol&nbs

*
Morphinone Morphinone is an opioid that is the intermediate when morphine is being converted to hydromorphone (trade name Dilaudid). Chemical structure Morphinone can be described as the ketone of morphine. Legal status Morphinone itself is an active ...
* Morphol&nbs

*
N-Phenethyl-14-ethoxymetopon ''N''-Phenethyl-14-ethoxymetopon is a drug that is a derivative of metopon. It is a potent analgesic, around 60 times stronger than morphine and produces significantly less constipation. ''N''-Phenethyl-14-ethoxymetopon acts as an agonist at bo ...
*
Noroxymorphone Noroxymorphone is an opioid which is both a metabolite of oxymorphone and oxycodone and is manufactured specifically as an intermediate in the production of narcotic antagonists such as naltrexone and others. It is a potent agonist of the μ-opi ...
*
Oxycodone Oxycodone, sold under various brand names such as Roxicodone and OxyContin (which is the extended release form), is a strong, semi-synthetic opioid used medically for treatment of moderate to severe pain. It is highly addictive and a commonly ...
*
Oxymorphol Oxymorphol is oxymorphone which has been hydrogenated at the 6-position and consists of a mixture of 4,5α-Epoxy-17-methylmorphinan-3,6β,14-triol and 4,5α-Epoxy-17-methylmorphinan-3,6α,14-triol (hydromorphinol). . It is produced by the human ...
*
Oxymorphone Oxymorphone (sold under the brand names Numorphan and Opana among others) is a highly potent opioid analgesic indicated for treatment of severe pain. Pain relief after injection begins after about 5–10 minutes, after oral administration it beg ...
* Pentamorphone * Semorphone


Morphides

* α-Chlorocodide (= chlorocodide)&nbs

* β-Chlorocodide&nbs

* α-Chloromorphide (= chloromorphide) * Bromocodide&nbs

* Bromomorphide&nbs

* Chlorodihydrocodide&nbs

* Chloromorphide * Codide 


Dihydrocodeine series

*
14-Hydroxydihydrocodeine 14-Hydroxydihydrocodeine (RAM-318) is an opiate analgesic drug, which is also an active metabolite of oxycodone and hydromorphinol. 14-Hydroxydihydrocodeine is not currently marketed in any developed country, but has been of interest to pharmaceu ...
*
Acetyldihydrocodeine Acetyldihydrocodeine is an opiate derivative discovered in Germany in 1914 and was used as a cough suppressant and analgesic. It is not commonly used, but has activity similar to other opiates. Acetyldihydrocodeine is a very close relative de ...
*
Dihydrocodeine Dihydrocodeine is a semi- synthetic opioid analgesic prescribed for pain or severe dyspnea, or as an antitussive, either alone or compounded with paracetamol (acetaminophen) (as in co-dydramol) or aspirin. It was developed in Germany in 1908 an ...
*
Dihydrodesoxycodeine Desocodeine is a semi-synthetic opioid which is the penultimate intermediate in the manufacture of desomorphine Desomorphine is a semi-synthetic opioid commercialized by Roche, with powerful, fast-acting effects, such as sedation and analgesia ...
 (desocodeine)  * Dihydroisocodeine  *
Nicocodeine Nicocodeine (Lyopect, Tusscodin) is an opioid analgesic and cough suppressant, an ester of codeine closely related to dihydrocodeine and the codeine analogue of nicomorphine. It is not commonly used in most countries, but has activity similar ...
*
Nicodicodeine Nicodicodine is an opioid developed as a cough suppressant and analgesic. Synthesized in 1904, it is not commonly used, but has activity similar to other opioids. Nicodicodine is metabolised in the liver by demethylation to produce 6-nicotinoyld ...


Nitrogen morphine derivatives

* 1-Nitrocodeine cas

*
Codeine-N-oxide Codeine-''N''-oxide (genocodeine) is an active metabolite of codeine. It is an opiate listed as a Schedule I controlled substance. It has a DEA ACSCN of 9053 and its annual manufacturing quota for 2013 was 602 grams. Like morphine-''N''-o ...
&nbs

*
Morphine-N-oxide Morphine-''N''-oxide (genomorphine) is an active opioid metabolite of morphine. Morphine itself, in trials with rats, is 11–22 times more potent than morphine-''N''-oxide subcutaneously and 39–89 times more potent intraperitoneally. However ...


Hydrazones

*
Oxymorphazone Oxymorphazone is an opioid analgesic drug related to oxymorphone. Oxymorphazone is a potent and long acting μ-opioid agonist which binds irreversibly to the receptor, forming a covalent bond which prevents it from detaching once bound. This gi ...


Halogenated morphine derivatives

* 1-Bromocodeine  * 1-Chlorocodeine  * 1-Iodomorphine *


Active opiate metabolites

* Codeine-6-glucuronide  *
Codeine-N-oxide Codeine-''N''-oxide (genocodeine) is an active metabolite of codeine. It is an opiate listed as a Schedule I controlled substance. It has a DEA ACSCN of 9053 and its annual manufacturing quota for 2013 was 602 grams. Like morphine-''N''-o ...
 (genocodein

* Heroin-7,8-oxide&nbs

*
Morphine-6-glucuronide Morphine-6-glucuronide (M6G) is a major active metabolite of morphine. M6G is formed from morphine by the enzyme UGT2B7. It has analgesic effects more potent than morphine. M6G can accumulate to toxic levels in kidney failure. History of discover ...
*
3-Monoacetylmorphine 3-Monoacetylmorphine (3-MAM) or 3-acetylmorphine is a less active metabolite of heroin (diacetylmorphine), the other two being morphine and more active 6-monoacetylmorphine 6-Monoacetylmorphine (6-MAM, 6-acetylmorphine, or 6-AM) is one of th ...
*
6-Monoacetylmorphine 6-Monoacetylmorphine (6-MAM, 6-acetylmorphine, or 6-AM) is one of three active metabolites of heroin (diacetylmorphine), the others being morphine and the much less active 3-monoacetylmorphine (3-MAM). Pharmacology 6-MAM occurs as a metabolite o ...
*
Morphine-N-oxide Morphine-''N''-oxide (genomorphine) is an active opioid metabolite of morphine. Morphine itself, in trials with rats, is 11–22 times more potent than morphine-''N''-oxide subcutaneously and 39–89 times more potent intraperitoneally. However ...
 (genomorphine) * Naltrexol&nbs

*
Norcodeine Norcodeine is an opiate analogue that is the N-demethylated derivative of codeine. It has relatively little opioid activity in its own right, but is formed as a metabolite of codeine following ingestion. Norcodeine is a Schedule I Narcotic cont ...
  *
Normorphine Normorphine is an opiate analogue, the N-demethylated derivative of morphine, that was first described in the 1950s when a large group of N-substituted morphine analogues were characterized for activity. The compound has relatively little opioid ...


Morphinan Morphinan is the prototype chemical structure of a large chemical class of psychoactive drugs, consisting of opiate analgesics, cough suppressants, and dissociative hallucinogens, among others. Structure Morphinan has a phenanthrene core stru ...
s


Morphinan series

* 3-Hydroxymorphinan  * 4-Chlorophenylpyridomorphinan&nbs

*
Cyclorphan Cyclorphan is an opioid analgesic of the morphinan family that was never marketed. It acts as a μ-opioid receptor (MOR) weak partial agonist or antagonist, κ-opioid receptor (KOR) full agonist, and, to a much lesser extent, δ-opioid receptor ...
* Levargorphan&nbs

*
Levorphanol Levorphanol (brand name Levo-Dromoran) is an opioid medication used to treat moderate to severe pain. It is the levorotatory enantiomer of the compound racemorphan. Its dextrorotatory counterpart is dextrorphan. It was first described in German ...
* Levophenacylmorphan *
Levomethorphan Levomethorphan (LVM) ( INN, BAN) is an opioid analgesic of the morphinan family that has never been marketed. It is the L-stereoisomer of racemethorphan (methorphan). The effects of the two isomers of the racemethorphan are quite different, with ...
*
Methorphan Methorphan comes in two isomeric forms, each with differing pharmacology and effects: * Dextromethorphan - An over-the-counter cough suppressant, as well as dissociative hallucinogen. * Levomethorphan - A potent opioid analgesic that was ne ...
 (racemethorphan) * Morphanol (racemorphanol) *
Norlevorphanol Norlevorphanol is an opioid analgesic of the morphinan family that was never marketed. It is the ''levo''- isomer of 3-hydroxymorphinan (morphinan-3-ol). Norlevorphanol is a Schedule I Narcotic controlled substance in the United States with an ...
* N-Methylmorphinan&nbs

* Oxilorphan *
Phenomorphan Phenomorphan is an opioid analgesic. It is not currently used in medicine, but has similar side-effects to other opiates, which include itching, nausea and respiratory depression. Phenomorphan is a highly potent drug due to the N-phenethyl group, ...
*
Proxorphan Proxorphan ( INN), also known as proxorphan tartate ( USAN) (developmental code name BL-5572M), is an opioid analgesic and antitussive drug of the morphinan family that was never marketed. It acts preferentially as a κ-opioid receptor partial a ...
*
Ro4-1539 Ro4-1539 (furethylnorlevorphanol) is an opioid analgesic drug from the morphinan series that was discovered by the pharmaceutical company Hoffmann–La Roche in the 1950s. It acts as a potent μ-opioid agonist, and was found to be around 30-60 t ...
* Stephodeline&nbs

Xorphanol Xorphanol (INN) (developmental code name TR-5379 or TR-5379M), also known as xorphanol mesylate (USAN), is an opioid analgesic of the morphinan family that was never marketed. Xorphanol is a mixed agonist–antagonist of opioid receptors, acti ...


Others

* 1-Nitroaknadinine * 14-episinomenine  * 5,6-Dihydronorsalutaridine  * 6-Keto Nalbuphine  * Aknadinine  *
Butorphanol Butorphanol is a morphinan-type synthetic agonist–antagonist opioid analgesic developed by Bristol-Myers. Butorphanol is most closely structurally related to levorphanol. Butorphanol is available as the tartrate salt in injectable, tablet, an ...
* Cephakicine  * Cephasamine  *
Cyprodime Cyprodime is an opioid antagonist from the morphinan family of drugs. Cyprodime is a selective opioid antagonist which blocks the μ-opioid receptor, but without affecting the δ-opioid or κ-opioid receptors. This makes it useful for scien ...
*
Drotebanol Drotebanol (Oxymethebanol) is a morphinan derivative that acts as an opioid agonist. It was invented by Daiichi Sankyo Co., Sankyo Company in Japan during the 1970s. It is synthesised from thebaine. Drotebanol has powerful antitussive (cough su ...
* Fenfangjine G  *
Ketorfanol Ketorfanol (International Nonproprietary Name, INN, United States Adopted Name, USAN) (developmental code name SBW-22), or ketorphanol, is an opioid analgesic of the morphinan family that was found to possess "potent antinociception, antiwrithing ...
*
Nalbuphine Nalbuphine, sold under the brand names Nubain among others, is an opioid analgesic which is used in the treatment of pain. It is given by injection into a vein, muscle, or fat. Side effects of nalbuphine include sedation, sweatiness, clammin ...
* Nalbuphone * Tannagine


Benzomorphan Benzomorphan is a chemical compound that is the base for a series of drugs which variably act on the opioid kappa and sigma receptors, including the following compounds: * 5,9-DEHB * 8-CAC * Alazocine * Anazocine * Bremazocine * Butinazocine ...
s

* 5,9 alpha-diethyl-2-hydroxybenzomorphan (5,9-DEHB)&nbs

*
8-Carboxamidocyclazocine 8-Carboxamidocyclazocine (8-CAC) is an opioid analgesic drug related to cyclazocine, discovered by medicinal chemist Mark P. Wentland and co-workers in Cogswell Laboratory at Rensselaer Polytechnic Institute. Similarly to cyclazocine, 8-CAC acts ...
 (8-CAC) *
Alazocine Alazocine (developmental code name -10047), also known more commonly as ''N''-allylnormetazocine (NANM), is a synthetic opioid analgesic of the benzomorphan family related to metazocine, which was never marketed. In addition to its opioid activ ...
* Anazocine&nbs

*
Bremazocine Bremazocine is a κ-opioid receptor agonist related to pentazocine. It has potent and long-lasting analgesic and diuretic effects. It has 200 times the activity of morphine, but appears to have no addictive properties and does not depress brea ...
*
Butinazocine Butinazocine (INN) is an opioid analgesic of the benzomorphan family which was never marketed. See also * Benzomorphan Benzomorphan is a chemical compound that is the base for a series of drugs which variably act on the opioid kappa and sig ...
&nbs

* Carbazocine&nbs

*
Cogazocine Cogazocine (INN) is an opioid analgesic of the benzomorphan family which was never marketed. See also * Benzomorphan Benzomorphan is a chemical compound that is the base for a series of drugs which variably act on the opioid kappa and sigma ...
*
Cyclazocine Cyclazocine is a mixed opioid agonist/antagonist related to dezocine, pentazocine and phenazocine. This family of opioid drugs is called the benzomorphans or benzazocines. It is a KOR agonist and MOR partial agonist, and also has high affinity ...
*
Dezocine Dezocine, sold under the brand name Dalgan, is an atypical opioid analgesic which is used in the treatment of pain. It is used by intravenous infusion and intramuscular injection. Dezocine is an opioid receptor modulator, acting as a partial ...
* Eptazocine *
Etazocine Etazocine (NIH-7856) is an opioid analgesic of the benzomorphan family which was never marketed. It acts as a partial agonist of the opioid receptors, with mixed agonist and receptor antagonist, antagonist effects. In animal studies, it was shown ...
&nbs

* Ethylketazocine&nbs

*
Fedotozine Fedotozine (INN; JO 1196 for the (-) tartrate salt) is an opioid drug of the arylacetamide series which acts as a peripherally specific selective κ1-opioid receptor agonist with preference for the κ1A subtype. It was under investigation f ...
 

* Fluorophen&nbs

*
Gemazocine Gemazocine (R-15,497), also known as cyclogemine, is a non-selective opioid antagonist of the benzomorphan class. It may have partial agonist properties at some of the opioid receptor Opioid receptors are a group of inhibitory G protein-coupled ...
&nbs

*
Ibazocine Ibazocine (INN, USAN) is an opioid analgesic which was never marketed. See also * Benzomorphan Benzomorphan is a chemical compound that is the base for a series of drugs which variably act on the opioid kappa and sigma receptors, including ...
&nbs

*
Ketazocine Ketazocine (INN), also known as ketocyclazocine, is a benzomorphan derivative used in opioid receptor research. Ketazocine, for which the receptor is named, is an exogenous opioid that binds to the κ opioid receptor. Activation of this receptor ...
*
Metazocine Metazocine is an opioid analgesic related to pentazocine. While metazocine has significant analgesic effects, mediated through a mixed agonist–antagonist action at the mu opioid receptor, its clinical use is limited by dysphoric and hallucino ...
*
Moxazocine Moxazocine (BL-4566) is an opioid analgesic of the benzomorphan family which was never marketed. It acts as a partial agonist or mixed agonist/antagonist of the opioid receptors and binds preferentially to the κ-opioid receptor. Despite its fail ...
 

*
Pentazocine Pentazocine, sold under the brand name Talwin among others, is a painkiller used to treat moderate to severe pain. It is believed to work by activating (agonizing) κ-opioid receptors (KOR) and μ-opioid receptors (MOR). As such it is called an ...
*
Phenazocine Phenazocine (brand names Prinadol, Narphen) is an opioid analgesic drug, which is related to pentazocine and has a similar profile of effects. Effects of phenazocine include analgesia and euphoria, also may include dysphoria and hallucinations at ...
* Quadazocine&nbs

* SKF-10047 * Thiazocine&nbs

* Tonazocine *
Volazocine Volazocine is an opioid analgesic of the benzomorphan class which was never marketed. Synthesis See also * Benzomorphan *ketazocine *cyclazocine Cyclazocine is a mixed opioid agonist/antagonist related to dezocine, pentazocine and phena ...
* Zenazocine


4-Phenylpiperidine 4-Phenylpiperidine is a chemical compound. It features a benzene ring bound to a piperidine ring. 4-Phenylpiperidine is the base structure for a variety of opioids, such as pethidine (meperidine), ketobemidone, alvimopan, loperamide, and diphen ...
s


Pethidine Pethidine, also known as meperidine and sold under the brand name Demerol among others, is a synthetic opioid analgesic, pain medication of the phenylpiperidine class. Synthesized in 1938 as a potential anticholinergic agent by the German chemis ...
s (meperidines)

* 4-Fluoropethidine * Allylnorpethidine *
Anileridine Anileridine (trade name: Leritine) is a synthetic analgesic drug and is a member of the piperidine class of analgesic agents developed by Merck & Co. in the 1950s. It differs from pethidine (meperidine) in that the ''N''-methyl group of meperidi ...
*
Benzethidine Benzethidine is a 4-phenylpiperidine derivative that is related to the clinically used opioid analgesic drug pethidine (''meperidine'', or ''Demerol''). Benzethidine is not currently used in medicine and is a Class A/ Schedule I drug which is c ...
* Carperidine *
Difenoxin Difenoxin (Motofen, R-15403) is an opioid drug used, often in combination with atropine, to treat diarrhea. It is the principal metabolite of diphenoxylate. It was first approved in the US in 1978 and in 1980 in the former West Germany. Difeno ...
*
Diphenoxylate Diphenoxylate is a centrally active opioid drug of the phenylpiperidine series that is used as a combination drug with atropine for the treatment of diarrhea. Diphenoxylate is an opioid and acts by slowing intestinal contractions; the atropine i ...
* Etoxeridine (carbetidine) *
Furethidine Furethidine is a 4-phenylpiperidine derivative that is related to the clinically used opioid analgesic drug pethidine (meperidine), but with around 25x higher potency. According to another source, Furethidine is 500/30 = 16.7 x the potency of pe ...
*
Hydroxypethidine Hydroxypethidine (Bemidone) is an opioid analgesic that is an analogue of the more commonly used pethidine (meperidine). Hydroxypethidine is slightly more potent than meperidine as an analgesic, 1.5x meperidine in potency, and it also has NMDA a ...
 (bemidone) * Morpheridine * Meperidine-N-oxide  *
Oxpheneridine OxpheneridineCS Patent 109234 is a 4-phenylpiperidine derivative that is related to the opioid analgesic drug pethidine (meperidine). Oxpheneridine is not currently used in medicine. Presumably it has similar effects to other opioid derivatives ...
 (carbamethidine) *
Pethidine Pethidine, also known as meperidine and sold under the brand name Demerol among others, is a synthetic opioid analgesic, pain medication of the phenylpiperidine class. Synthesized in 1938 as a potential anticholinergic agent by the German chemis ...
 (meperidine) *
Pethidine intermediate A Pethidine intermediate A is a 4-phenylpiperidine derivative that is a precursor to the opioid analgesic drug pethidine (meperidine). It is not known to have any analgesic activity in its own right, however other derivatives of pethidine with a 4 ...
*
Pethidine intermediate B Norpethidine (normeperidine, pethidine intermediate B) is a 4-phenylpiperidine derivative that is both a precursor to, and the toxic metabolite of, pethidine (meperidine). It is scheduled by UN Single Convention on Narcotic Drugs. It is a Sch ...
 (norpethidine) *
Pethidine intermediate C Pethidinic acid (meperidinic acid, pethidine intermediate C) is a 4-phenylpiperidine derivative that is both a metabolite of and a precursor to pethidine (meperidine). It is scheduled by UN Single Convention on Narcotic Drugs. It is a Schedule ...
 (pethidinic acid) * Pheneridine *
Phenoperidine Phenoperidine(Operidine or Lealgin), is an opioid analgesic which is structurally related to pethidine and is used clinically as a general anesthetic. Medical use Phenoperidine is an opioid pain killer -- narcotic analgesic. Pharmacology It i ...
*
Piminodine Piminodine (Alvodine) is an opioid analgesic that is an analog (chemistry), analogue of pethidine (meperidine). It was used in medicine briefly during the 1960s and 70s, but has largely fallen out of clinical use. It was used particularly for ob ...
* Properidine (ipropethidine) * Sameridine


Prodine Prodine (trade names Prisilidine and Nisentil) is an opioid analgesic that is an analog of pethidine (meperidine). It was developed in Germany in the late 1940s. There are two isomers of the trans form of prodine, alphaprodine and betaprodine ...
s

*
Allylprodine Allylprodine is an opioid analgesic that is an analog of prodine. It was discovered by Hoffman-La Roche in 1957 during research into the related drug pethidine. Derivatives were tested to prove the theory that phenolic & non-phenolic opioids bi ...
* (α/β)- Meprodine *
Desmethylprodine Desmethylprodine or 1-methyl-4-phenyl-4-propionoxypiperidine (MPPP, Ro 2-0718) is an opioid analgesic drug developed in the 1940s by researchers at Hoffmann-La Roche. Desmethylprodine has been labeled by the Drug Enforcement Administration, DE ...
 (MPPP) *
PEPAP PEPAP (phenethylphenylacetoxypiperidine) is an opioid analgesic that is an analog (chemistry), analog of pethidine (meperidine). It is related to the drug MPPP, with an ''N''-phenethyl group in place of the ''N''-methyl substitution and an ace ...
* (α/β)-
Prodine Prodine (trade names Prisilidine and Nisentil) is an opioid analgesic that is an analog of pethidine (meperidine). It was developed in Germany in the late 1940s. There are two isomers of the trans form of prodine, alphaprodine and betaprodine ...
* Prosidol *
Trimeperidine Trimeperidine (Promedol) is an opioid analgesic that is an analogue of prodine. It was developed in the early 1950s in the USSR during research into the related drug pethidine. Trimeperidine has four structural isomers, of which two are acti ...
 (promedol)


Ketobemidone Ketobemidone, sold under the brand name Ketogan among others, is a powerful synthetic opioid painkiller. Its effectiveness against pain is in the same range as morphine, and it also has some NMDA-antagonist properties imparted, in part, by its m ...
s

*
Acetoxyketobemidone Acetoxyketobemidone (O-Acetylketobemidone) is an opioid analgesic that is an acetylated derivative of ketobemidone. It was developed in the 1950s during research into analogues of pethidine and was assessed by the United Nations Office on Drugs a ...
* Droxypropine *
Ketobemidone Ketobemidone, sold under the brand name Ketogan among others, is a powerful synthetic opioid painkiller. Its effectiveness against pain is in the same range as morphine, and it also has some NMDA-antagonist properties imparted, in part, by its m ...
*
Methylketobemidone Methylketobemidone is an opioid analgesic that is an analogue of ketobemidone. It was developed in the 1950s during research into analogues of pethidine and was assessed by the United Nations Office on Drugs and Crime but was not included on the ...
*
Propylketobemidone Propylketobemidone is an opioid analgesic that is an analogue of ketobemidone. It was developed in the 1950s during research into analogues of pethidine and was assessed by the United Nations Office on Drugs and Crime but was not included on the ...


Others

*
Alvimopan Alvimopan (trade name Entereg) is a drug which behaves as a peripherally acting μ-opioid receptor antagonist. With the limited ability to cross the blood–brain barrier and reach the μ-opioid receptors of the central nervous system, the clin ...
*
Loperamide Loperamide, sold under the brand name Imodium, among others,Drugs.co Page accessed September 4, 2015 is a medication used to decrease the frequency of diarrhea. It is often used for this purpose in inflammatory bowel disease and short bowel synd ...
* LS-115509 * Picenadol


Open chain In chemistry, an open-chain compound (also spelled as open chain compound) or acyclic compound (Greek prefix "α", ''without'' and "κύκλος", ''cycle'') is a compound with a linear structure, rather than a cyclic one. An open-chain compound h ...
opioids


Amidones

* Dextromethadone&nbs

*
Dipipanone Dipipanone (Pipadone) is a strong opioid analgesic drug, used for acute pain by mouth (PO) for adults - initially 10 mg every 6 hours, then increased if necessary up to 30 mg every 6 hours, with the dose to be increased gradually. It is often use ...
* Isomethadone&nbs

* Levoisomethadone  * Levomethadone  *
Methadone Methadone, sold under the brand names Dolophine and Methadose among others, is a synthetic opioid agonist used for chronic pain and also for opioid dependence. It is used to treat chronic pain, and it is also used to treat addiction to heroin ...
*
Methadone intermediate Methadone intermediate is a methadone precursor scheduled by UN Single Convention on Narcotic Drugs. It is a Schedule II Narcotic controlled substance in the United States and has an ACSCN of 9254. The 2014 annual manufacturing quota was 32 ...
&nbs

* Normethadone * Norpipanone&nbs

*
Phenadoxone Phenadoxone (trade names Heptalgin, Morphidone, and Heptazone) is an opioid analgesic of the open chain class (methadone and relatives) invented in Germany by Hoechst in 1947. It is one of a handful of useful synthetic analgesics which were used ...
 (heptazone)


Methadols

*
Acetylmethadol Acetylmethadol, also known as methadyl acetate, is a synthetic opioid analgesic. It is a racemic mixture of alphacetylmethadol (α-acetylmethadol) and betacetylmethadol (β-acetylmethadol), which are in turn racemic mixtures of levacetylmethado ...
  * Alphaacetylmethadol  *
Alphamethadol Alphamethadol ( INN), or α-methadol, also known as alfametadol, is a synthetic opioid analgesic. It is an isomer of dimepheptanol (methadol), the other being betamethadol (β-methadol). Alphamethadol is composed of two isomers itself, L-α-met ...
  *
Betacetylmethadol Betacetylmethadol is a Chemical synthesis, synthetic opioid. It is a diastereoisomer of alphacetylmethadol (as well as levacetylmethadol). In the United States, betacetylmethadol is a List of Schedule I drugs (US), Schedule I drug Narcotic under ...
  *
Betamethadol Betamethadol ( INN), or β-methadol, also known as betametadol, is a synthetic opioid analgesic. It is an isomer of dimepheptanol (methadol), the other being alphamethadol (α-methadol). Betamethadol is composed of two isomers itself, L-β-meth ...
  *
Dimepheptanol Dimepheptanol (International nonproprietary name, INN; Amidol, Pangerin), also known as methadol or racemethadol, is a Chemical synthesis, synthetic opioid analgesic related to methadone. It has similar effects to other opioids, including Analge ...
 (racemethadol) * Isomethadol  *
Levacetylmethadol Levacetylmethadol (INN), levomethadyl acetate (USAN), OrLAAM (trade name) or levo-α-acetylmethadol (LAAM) is a synthetic opioid similar in structure to methadone. It has a long duration of action due to its active metabolites. Medical uses LAA ...
*
Noracymethadol Noracymethadol (INN) is a synthetic opioid analgesic related to methadone that was never marketed. In a clinical trial of postpartum patients it was reported to produce analgesia comparable to that of morphine but with less nausea, dizziness ...


Moramides

* Desmethylmoramide  *
Dextromoramide Dextromoramide (Palfium, Palphium, Jetrium, Dimorlin) is a powerful opioid analgesic approximately three times more potent than morphine but shorter acting. It is subject to drug prohibition regimes, both internationally through UN treaties and b ...
*
Levomoramide Levomoramide is the inactive isomer of the opioid analgesic dextromoramide, invented by the chemist Paul Janssen in 1956. Unlike dextromoramide, which is a potent analgesic with high abuse potential, levomoramide is virtually without activity. ...
*
Moramide intermediate Moramide intermediate (3-methyl-4-morpholin-4-yl-2,2-diphenylbutanoic acid, on INCB Yellow List as 2-methyl-3-morpholino-1,1-diphenylpropane carboxylic acid) is a moramide precursor scheduled by UN Single Convention on Narcotic Drugs. In the U ...
 

*
Racemoramide Racemoramide (INN, BAN), or simply moramide, is an opioid analgesic and a racemic mixture of the substances dextromoramide (the active component) and levomoramide (which is inactive), two enantiomers of a chiral molecule. Racemoramide is it ...


Thiambutene The Thiambutenes are a family of opioid analgesic drugs developed at the British research laboratory of Burroughs-Wellcome in the late 1940s. The parent compound thiambutene has no analgesic effects, but several compounds from this group are anal ...
s

*
Diethylthiambutene Diethylthiambutene (Thiambutene, Themalon, Diethibutin, ''N'',''N''-Diethyl-1-methyl-3,3-di-2-thienylallylamine) is an opioid analgesic drug developed in the 1950s which was mainly used as an anesthetic in veterinary Veterinary medicine is th ...
* Dimethylthiambutene *
Ethylmethylthiambutene Ethylmethylthiambutene (; Emethibutin) is an opioid analgesic drug from the thiambutene family, around 1.3x the potency of morphine Morphine is a strong opiate that is found naturally in opium, a dark brown resin in poppies ('' Papaver ...
*
Piperidylthiambutene Piperidylthiambutene (Piperidinohton) is a synthetic opioid analgesic drug from the thiambutene family, which has around the same potency as morphine. Piperidylthiambutene is structurally distinct from fentanyl, its analogues, and other syntheti ...
*
Pyrrolidinylthiambutene Pyrrolidinylthiambutene is an opioid analgesic drug from the thiambutene family with around 3/4 of the potency of morphine Morphine is a strong opiate that is found naturally in opium, a dark brown resin in poppies ('' Papaver somniferu ...
*
Thiambutene The Thiambutenes are a family of opioid analgesic drugs developed at the British research laboratory of Burroughs-Wellcome in the late 1940s. The parent compound thiambutene has no analgesic effects, but several compounds from this group are anal ...


Phenalkoxams

*
Dextropropoxyphene Dextropropoxyphene is an analgesic in the opioid category, patented in 1955 and manufactured by Eli Lilly and Company. It is an optical isomer of levopropoxyphene. It is intended to treat mild pain and also has antitussive (cough suppressant) a ...
 (propoxyphene) * Dimenoxadol * Dioxaphetyl butyrate *
Levopropoxyphene Levopropoxyphene is an antitussive. It is an optical isomer of dextropropoxyphene. The racemic mixture is called propoxyphene. Only the dextro-isomer (dextropropoxyphene) has an analgesic effect; the levo-isomer appears to exert only an antitussi ...
* Norpropoxyphene * Pyrroliphene


Ampromides

*
Diampromide Diampromide is an opioid analgesic from the ampromide family of drugs, related to other drugs such as propiram and phenampromide. It was invented in the 1960s by American Cyanamid, and can be described as a ring-opened analogue of fentanyl. Diamp ...
*
Phenampromide Phenampromide is an opioid analgesic from the ampromide family of drugs, related to other drugs such as propiram and diampromide. It was invented in the 1960s by American Cyanamid Co. Although never given a general release, it was trialled and ...
*
Propiram Propiram (Algeril, Dirame, Bay 4503) is a partial mu opioid receptor agonist and weak mu antagonist analgesic from the ampromide family of drugs related to other drugs such as phenampromide and diampromide. It was invented in 1963 in the United ...


Others

*
Embutramide Embutramide (International Nonproprietary Name, INN, United States Adopted Name, USAN, British Approved Name, BAN) (brand name Embutane) is a potent opioid analgesic and sedative drug that is structurally related to methadone. It was developed by ...
*
IC-26 IC-26 (WIN 1161-3, Methiodone) is an analogue of the opioid analgesic methadone, where the carbonyl group has been replaced by the bioisosteric sulfone group. Human and animal studies suggest that IC-26 is around the same potency as methadone ...
*
Isoaminile Isoaminile is an antitussive (cough suppressant) used under the trade-name Peracon. The normal therapeutic dose is 40–80 mg of the cyclamate salt, with a maximum of five doses in a 24-hour period. In addition to its central antitussive ...
*
Lefetamine Lefetamine (Santenol) is a drug which is a stimulant and also an analgesic with effects comparable to codeine. Discovery Lefetamine-related 1,2-diphenylethylamines were invented in the 1940s and showed weak analgesic activity. It was inv ...
* R-4066


Anilidopiperidines

* 3-Allylfentanyl * 3-Methylfentanyl * 3-Methylthiofentanyl * 4-Phenylfentanyl *
Alfentanil Alfentanil (R-39209, trade name Alfenta, Rapifen in Australia) is a potent but short-acting synthetic opioid analgesic drug, used for anaesthesia in surgery. It is an analogue of fentanyl with around one-fourth to one-tenth the potency, one-third ...
* α-Methylacetylfentanyl *
α-Methylfentanyl α-Methylfentanyl (or ''alpha''-Methylfentanyl) an opioid analgesic that is an analog of fentanyl. It is sometimes sold as "China White". History α-Methylfentanyl was discovered by a team at Janssen Pharmaceutica in the 1960s. In 1976, it be ...
* α-Methylthiofentanyl *
Benzylfentanyl Benzylfentanyl (R-4129) is a fentanyl analog. It was temporarily placed in the US Schedule I by emergency scheduling in 1985 due to concerns about its potential for abuse as a designer drug, but this placement was allowed to expire and benzylfen ...
&nbs

nbsp; * β-hydroxyfentanyl * β-hydroxythiofentanyl * β-Methylfentanyl * Brifentanil *
Butyrfentanyl Butyrfentanyl or butyrylfentanyl is a potent short-acting synthetic opioid analgesic drug. It is an analog of fentanyl with around one quarter of its potency. One of the first mentions of this drug can be found in document written by The Colleg ...
*
Carfentanil Carfentanil or carfentanyl, sold under the brand name Wildnil, is a very potent opioid analgesic which is used in veterinary medicine to anesthetize large animals such as elephants and rhinoceroses. It is typically administered in this context ...
*
Fentanyl Fentanyl, also spelled fentanil, is a very potent synthetic opioid used as a pain medication. Together with other drugs, fentanyl is used for anesthesia. It is also used illicitly as a recreational drug, sometimes mixed with heroin, cocaine ...
*
Lofentanil Lofentanil is one of the most potent opioid analgesics known and is an analogue of fentanyl, which was developed in 1960. It is most similar to the highly potent opioid carfentanil (4-carbomethoxyfentanyl), only slightly more potent. Lofentanil ...
*
N-Methylcarfentanil ''N''-Methylnorcarfentanil (R-32395) is an opioid analgesic drug related to the highly potent animal tranquilizer carfentanil, but several thousand times weaker, being only slightly stronger than morphine. It was first synthesised by a team of c ...
* Mirfentanil * Ocfentanil *
Ohmefentanyl Ohmefentanyl (also known as β-hydroxy-3-methylfentanyl, OMF and RTI-4614-4) is an extremely potent opioid analgesic drug which selectively binds to the µ-opioid receptor. There are eight possible stereoisomers of ohmefentanyl. These stereois ...
*
Parafluorofentanyl Parafluorofentanyl (4-fluorofentanyl, pFF) is an opioid analgesic analogue of fentanyl developed by Janssen Pharmaceutica in the 1960s. 4-Fluorofentanyl was sold briefly on the US black market in the early 1980s, before the introduction of the ...
* Phenaridine * R-30490 *
Remifentanil Remifentanil is a potent, short-acting synthetic opioid analgesic drug. It is given to patients during surgery to relieve pain and as an adjunct to an anaesthetic. Remifentanil is used for sedation as well as combined with other medications fo ...
*
Sufentanil Sufentanil, sold under the brand names Dsuvia and Sufenta, is a synthetic opioid analgesic drug approximately 5 to 10 times as potent as its parent drug, fentanyl, and 500 times as potent as morphine. Structurally, sufentanil differs from fen ...
* Thenylfentanyl&nbs

* * Thiofentanyl * Trefentanil


Oripavine Oripavine is an opioid and the major metabolite of thebaine. It is the parent compound from which a series of semi-synthetic opioids are derived, which includes the compounds etorphine and buprenorphine. Although its analgesic potency is compar ...
derivatives

*
7-PET 7-PET is an opioid analgesic drug that has 300 times the potency of morphine by weight. It was discovered by K.W. Bentley and is related to the more well known oripavine derivative etorphine, which is used as a veterinary painkiller and anestheti ...
*
Acetorphine Acetorphine is a potent opioid analgesic, up to 8700 times stronger than morphine by weight. It is a derivative of the more well-known opioid etorphine, which is used as a very potent veterinary painkiller and anesthetic medication, primarily f ...
* Alletorphine (N-allyl-noretorphine) * BU-48 *
Buprenorphine Buprenorphine is an opioid used to treat opioid use disorder, acute pain, and chronic pain. It can be used under the tongue (sublingual), in the cheek (buccal), by injection (intravenous and subcutaneous), as a skin patch (transdermal), ...
*
Buprenorphine-3-glucuronide Buprenorphine-3-glucuronide (B3G) is a major active metabolite of the opioid modulator buprenorphine. It has affinity for the μ-opioid receptor (Ki = 4.9 (± 2.7) pM), δ-opioid receptor (Ki = 270 nM), and nociceptin receptor (Ki = 36 μM), but ...
* Cyprenorphine *
Dihydroetorphine Dihydroetorphine was developed by K. W. Bentley at McFarlan-Smith in the 1960s and is a potent opioid analgesic used mainly in China. It is a derivative of the better-known opioid etorphine, a very potent veterinary painkiller and anesthetic med ...
*
Etorphine Etorphine (M99) is a semi-synthetic opioid possessing an analgesic potency approximately 1,000–3,000 times that of morphine. It was first prepared in 1960 from oripavine, which does not generally occur in opium poppy extract but rather the r ...
* Homprenorphine * 18,19-Dehydrobuprenorphine (HS-599)&nbs

* N-cyclopropylmethylnoretorphine&nbs

* Nepenthone&nbs

*
Norbuprenorphine Norbuprenorphine is a major active metabolite of the opioid modulator buprenorphine. It is a μ-opioid, δ-opioid, and nociceptin receptor full agonist, and a κ-opioid receptor partial agonist. In rats, unlike buprenorphine, norbuprenorphine ...
*
Norbuprenorphine-3-glucuronide Norbuprenorphine-3-glucuronide (N3G) is a major active metabolite of the opioid modulator buprenorphine. It has affinity for the κ-opioid receptor (Ki = 300 nM) and the nociceptin receptor (Ki = 18 μM), but not for the μ- or δ-opioid recept ...
* Thevinone&nbs

* Thienorphinebr>


Phenazepanes

*
Ethoheptazine Ethoheptazine (trade name Zactane) is an opioid analgesic from the phenazepane family. It was invented in the 1950s and is a ring expanded analogue of pethidine. Ethoheptazine produces similar effects to other opioids, including analgesia, sedat ...
*
Meptazinol Meptazinol (trade name Meptid) is an opioid analgesic developed by Wyeth in the 1970s. Indications for use in moderate to severe pain, most commonly used to treat pain in obstetrics (childbirth). Meptazinol is a 3-phenylazepane derivative, wher ...
* Metheptazine * Metethoheptazine *
Proheptazine Proheptazine is an opioid analgesic from the phenazepine family. It was invented in the 1960s. Proheptazine produces similar effects to other opioids, including analgesia, sedation, euphoria, dizziness and nausea Nausea is a diffuse sensat ...


Pirinitramides

*
Bezitramide Bezitramide is an opioid analgesic. Bezitramide itself is a prodrug which is readily hydrolyzed in the gastrointestinal tract to its active metabolite, despropionyl-bezitramide. Bezitramide was discovered at Janssen Pharmaceutica in 1961. It is m ...
* Piritramide


Benzimidazole Benzimidazole is a heterocyclic aromatic organic compound. This bicyclic compound may be viewed as fused rings of the aromatic compounds benzene and imidazole. It is a colorless solid. Preparation Benzimidazole is produced by condensation of o- ...
s

*
Clonitazene Clonitazene is an opioid analgesic of approximately three times the potency of morphine. It is related to etonitazene Etonitazene is an analgesic drug, first reported in 1957, that has been shown to have approximately 1,000 to 1,500 times the po ...
*
Etonitazene Etonitazene is an analgesic drug, first reported in 1957, that has been shown to have approximately 1,000 to 1,500 times the potency of morphine in animals. Because it is characterized by a strong dependency potential and a tendency to produce pr ...
*
Isotonitazene Isotonitazene is a benzimidazole derived opioid analgesic drug related to etonitazene, which has been sold as a designer drug. It has only around half the potency of etonitazene in animal studies, but it is likely even less potent in humans as ...
*
Metonitazene Metonitazene is an analgesic compound related to etonitazene, which was first reported in 1957, and has been shown to have approximately 100 times the potency of morphine by central routes of administration, but if used orally it has been shown t ...


Indole Indole is an aromatic heterocyclic organic compound with the formula C8 H7 N. It has a bicyclic structure, consisting of a six-membered benzene ring fused to a five-membered pyrrole ring. Indole is widely distributed in the natural environmen ...
s

*
18-Methoxycoronaridine 18-Methoxycoronaridine (18-MC, or MM-110) is a derivative of ibogaine invented in 1996 by the research team around the pharmacologist Stanley D. Glick from the Albany Medical College and the chemists Upul K. Bandarage and Martin E. Kuehne fro ...
* 7-Acetoxymitragynine  *
7-Hydroxymitragynine 7-Hydroxymitragynine is a terpenoid indole alkaloid from the plant ''Mitragyna speciosa'', commonly known as Kratom. It is often referred to as ‘7-OH’. It was first described in 1994 and is a natural product derived from the mitragynine prese ...
* ψ-Akuammigine * Akuammidine  *
Akuammine Akuammine (vincamajoridine) is an indole alkaloid. It is the most abundant alkaloid found in the seeds from the tree ''Picralima nitida'', commonly known as akuamma, comprising 0.56% of the dried powder. It has also been isolated from ''Vinca ma ...
*
Coronaridine Coronaridine, also known as 18-carbomethoxyibogamine, is an alkaloid found in ''Tabernanthe iboga'' and related species, including ''Tabernaemontana divaricata'' for which (under the now obsolete synonym ''Ervatamia coronaria'') it was named. Li ...
*
Eseroline Eseroline is a drug which acts as an opioid agonist. It is a metabolite of the acetylcholinesterase inhibitor physostigmine but unlike physostigmine, the acetylcholinesterase inhibition produced by eseroline is weak and easily reversible, and it ...
*
Hodgkinsine Hodgkinsine is an alkaloid found in plants of the genus ''Psychotria'', particularly '' Psychotria colorata'', although it is also found in ''Psychotria lyciiflora'' and probably other species in this family, Hodgkinsine has antiviral, antibact ...
*
Ibogaine Ibogaine is a naturally occurring psychoactive substance found in plants in the family Apocynaceae such as ''Tabernanthe iboga'', ''Voacanga africana'', and ''Tabernaemontana undulata''. It is a psychedelic with dissociative properties. Prel ...
*
Mitragynine Mitragynine is an indole-based alkaloid and the most abundant active alkaloid in the Southeast Asian plant ''Mitragyna speciosa'', commonly known as '' kratom.'' The total alkaloid concentration in dried leaves ranges from 0.5 to 1.5%. In Thai va ...
* Mitragynine pseudoindoxyl *
Noribogaine Noribogaine (actually O-desmethylibogaine), or 12-hydroxyibogamine, is the principal psychoactive metabolite of the oneirogen ibogaine. It is thought to be involved in the antiaddictive effects of ibogaine-containing plant extracts, such as '' ...
*
Pericine Pericine is one of a number of indole alkaloids found in the tree '' Picralima nitida'', commonly known as akuamma. As with some other alkaloids from this plant such as akuammine, pericine has been shown to bind to mu opioid receptors ''in vitro ...
* Pseudoakuammigine


Beta Beta (, ; uppercase , lowercase , or cursive ; grc, βῆτα, bē̂ta or ell, βήτα, víta) is the second letter of the Greek alphabet. In the system of Greek numerals, it has a value of 2. In Modern Greek, it represents the voiced labiod ...
-
Amino In chemistry, amines (, ) are compounds and functional groups that contain a basic nitrogen atom with a lone pair. Amines are formally derivatives of ammonia (), wherein one or more hydrogen atoms have been replaced by a substituent s ...
Ketone In organic chemistry, a ketone is a functional group with the structure R–C(=O)–R', where R and R' can be a variety of carbon-containing substituents. Ketones contain a carbonyl group –C(=O)– (which contains a carbon-oxygen double bo ...
s

* 3-(dimethylamino)-2,2-dimethyl-1-phenylpropan-1-one


Diphenylmethylpiperazine 1-(Diphenylmethyl)piperazine, also known as benzhydrylpiperazine, is a chemical compound and piperazine derivative. It features a piperazine ring with a benzhydryl (diphenyl methyl) group bound to one of the nitrogen Nitrogen is the chemical ...
s

*
BW373U86 (+)-BW373U86 is an opioid analgesic drug used in scientific research. BW373U86 is a selective agonist for the δ-opioid receptor, with approximately 15x stronger affinity for the δ-opioid than the μ-opioid receptor The μ-opioid recep ...
*
DPI-221 DPI-221 is an opioid drug that is used in scientific research. It is a highly selective agonist for the Delta opioid receptor, δ-opioid Receptor (biochemistry), receptor, which produces fewer convulsions than most drugs from this family. Refer ...
*
DPI-287 DPI-287 is an opioid drug that is used in scientific research. It is a highly selective agonist for the δ-opioid receptor, which produces less convulsions than most drugs from this family. It has antidepressant Antidepressants are a class ...
*
DPI-3290 DPI-3290 was discovered by scientists at Burroughs Wellcome and licensed to Delta Pharmaceutical and is a drug that is used in scientific research. It is a potent analgesic drug, which produces little respiratory depression. DPI-3290 acts as a ...
*
SNC-80 SNC-80 is an opioid analgesic compound that selectively activates μ–δ opioid receptor heteromers and is used in scientific research. It was discovered in 1994. SNC-80 was the first non-peptide compound developed that was regarded as a high ...
* AZD-2327


Opioid peptide Opioid peptides are peptides that bind to opioid receptors in the brain; opiates and opioids mimic the effect of these peptides. Such peptides may be produced by the body itself, for example endorphins. The effects of these peptides vary, but t ...
s


Dynorphin Dynorphins (Dyn) are a class of opioid peptides that arise from the precursor protein prodynorphin. When prodynorphin is cleaved during processing by proprotein convertase 2 (PC2), multiple active peptides are released: dynorphin A, dynorphin B, a ...
s

*
Big dynorphin Big dynorphin is an endogenous opioid peptide of the dynorphin family that is composed of both dynorphin A and dynorphin B. Big dynorphin has the amino acid sequence Protein primary structure is the linear sequence of amino acids in a peptide or ...
*
Dynorphin A Dynorphin A is a dynorphin, an endogenous opioid peptide with the amino acid sequence: Tyr-Gly-Gly-Phe-Leu-Arg-Arg-Ile-Arg-Pro-Lys-Leu-Lys. Dynorphin A1–8 is a truncated form of dynorphin A with the amino acid sequence: Tyr-Gly-Gly-Phe-Leu-Ar ...
*
Dynorphin B Dynorphin B, also known as rimorphin, is a form of dynorphin and an endogenous opioid peptide with the amino acid sequence Tyr-Gly-Gly-Phe-Leu-Arg-Arg-Gln-Phe-Lys-Val-Val-Thr. Dynorphin B is generated as a proteolytic cleavage product of leumorph ...
*
Leumorphin Leumorphin, also known as dynorphin B1–29, is a naturally occurring endogenous opioid peptide. Derived as a proteolytic cleavage product of residues 226-254 of prodynorphin (preproenkephalin B), leumorphin is a nonacosapeptide (29 amino acid ...


Endomorphin Endomorphins are considered to be natural opioid neurotransmitters central to pain relief. The two known endomorphins, endomorphin-1 and endomorphin-2, are tetrapeptides, consisting of Tyr-Pro-Trp-Phe and Tyr-Pro-Phe-Phe amino acid sequences resp ...
s

* Endomorphin-1 * Endomorphin-2


Endorphin Endorphins (contracted from endogenous morphine) are chemical signals in the brain that block the perception of pain and increase feelings of wellbeing. They are produced and stored in an area of the brain known as the pituitary gland. Hist ...
s

*
α-Endorphin α-Endorphin is an endogenous opioid peptide with a length of 16 amino acids, and the amino acid sequence: Tyr- Gly-Gly- Phe- Met- Thr- Ser- Glu- Lys-Ser- Gln-Thr- Pro- Leu- Val-Thr. With the use of mass spectrometry, Nicholas Ling was able to ...
*
β-Endorphin ''beta''-Endorphin (β-endorphin) is an endogenous opioid neuropeptide and peptide hormone that is produced in certain neurons within the central nervous system and peripheral nervous system. It is one of three endorphins that are produced in ...
*
γ-Endorphin γ-Endorphin (''gamma''-endorphin) is an opioid peptide that is characterized by the presence of 17 amino acids. The first 16 amino acids are identical to α-endorphin; leucine added at the end. In addition, γ-endorphin is identical to the fir ...
* α-Neoendorphin * β-Neoendorphin


Enkephalin An enkephalin is a pentapeptide involved in regulating nociception in the body. The enkephalins are termed endogenous ligands, as they are internally derived and bind to the body's opioid receptors. Discovered in 1975, two forms of enkephalin ...
s

*
DADLE DADLE ( D-Ala2,_D-Leu5.html" ;"title="small>D-Ala2, D-Leu5">small>D-Ala2, D-Leu5Enkephalin) is a synthetic opioid peptide with analgesic properties. Although it is often considered a selective delta opioid receptor agonist, it also binds to the μ ...
*
DAMGO DAMGO ( D-Ala2,_''N''-MePhe4,_Gly-ol.html" ;"title="small>D-Ala2, ''N''-MePhe4, Gly-ol">small>D-Ala2, ''N''-MePhe4, Gly-olenkephalin) is a synthetic opioid peptide with high μ-opioid receptor specificity. It was synthesized as a biologically stab ...
*
Deltorphin Deltorphin, also known as deltorphin A and dermenkephalin, is a natural product, naturally occurring, exogenous opioid peptide, opioid heptapeptide and thus, exorphin, with the amino acid sequence Tyr-D-Met-Phe-His-Leu-Met-Asp-NH2. Along with the ...
&nbs

*
Met-enkephalin Met-enkephalin, also known as metenkefalin (INN), sometimes referred to as opioid growth factor (OGF), is a naturally occurring A natural product is a natural compound or substance produced by a living organism—that is, found in nature. In ...
*
Leu-enkephalin Leu-enkephalin is an endogenous opioid peptide neurotransmitter with the amino acid sequence Tyr-Gly-Gly-Phe-Leu that is found naturally in the brains of many animals, including humans. It is one of the two forms of enkephalin; the other is met-e ...


Propeptides

*
Proenkephalin Introduction Proenkephalin (PENK), formerly known as proenkephalin A (since proenkephalin B was renamed prodynorphin), is an endogenous opioid polypeptide hormone which, via proteolyic cleavage, produces the enkephalin peptides etnkephal ...
* Proendorphin *
Proopiomelanocortin Pro-opiomelanocortin (POMC) is a precursor polypeptide with 241 amino acid residues. POMC is synthesized in corticotrophs of the anterior pituitary from the 267-amino-acid-long polypeptide precursor pre-pro-opiomelanocortin (pre-POMC), by the r ...


Others / unknown

*
Adrenorphin Adrenorphin, also sometimes referred to as metorphamide, is an endogenous, C-terminally amidated, opioid octapeptide (Tyr-Gly-Gly-Phe-Met-Arg-Arg-Val-NH2, YGGFMRRV-NH2) that is produced from proteolytic cleavage of proenkephalin A and is wid ...
*
Amidorphin Amidorphin is an endogenous, C-terminally amidated, opioid peptide generated as a cleavage product of proenkephalin A in some mammalian species; in humans and most other species, the peptide is 1 residue longer and is not amidated. Amidorphin ...
* Biphalin *
Casokefamide Casokefamide ( INN), also known as β-casomorphin 4027 (β-CM-4027) and D-Ala2,4,Tyr5.html" ;"title="small>D-Ala2,4,Tyr5">small>D-Ala2,4,Tyr5β-casomorphin-5-amide, is a peripherally-specific, synthetic opioid pentapeptide with the amino acid s ...
*
Casomorphin Casomorphin is an opioid peptide (protein fragment) derived from the digestion of the milk protein casein. Health Digestive enzymes can break casein down into peptides that have some biological activity in cells and in laboratory animals though ...
s * Cytochrophin-4 *
DALDA Dalda is a brand of vegetable oil (hydrogenated vegetable cooking oil) popular in South Asia. History An individual by the name Hussein Dada, used to import vanaspati ghee from a Dutch company before the 1930s as a cheap substitute for des ...
( Tyr- D-
Arg Arg or ARG may refer to: Places *''Arg'' () means "citadel" in Persian, and may refer to: **Arg, Iran, a village in Fars Province, Iran **Arg (Kabul), presidential palace in Kabul, Afghanistan **Arg, South Khorasan, a village in South Khorasan P ...
- Phe- Lys- NH2br>
*
Deltorphin I Deltorphin I, also known as -Ala2eltorphin I or deltorphin C, is a natural product, naturally occurring, exogenous opioid peptide, opioid heptapeptide and hence, exorphin, with the amino acid sequence Tyr-D-Ala-Phe-Asp-Val-Val-Gly-NH2. While n ...
*
Deltorphin II Deltorphin, also known as deltorphin A and dermenkephalin, is a naturally occurring, exogenous opioid heptapeptide and thus, exorphin, with the amino acid sequence Tyr-D-Met-Phe-His-Leu-Met-Asp-NH2. Along with the other deltorphins (such as delt ...
* Deprolorphin *
Dermorphin Dermorphin is a hepta-peptide first isolated from the skin of South American frogs belonging to the genus ''Phyllomedusa''. The peptide is a natural opioid that binds as an agonist with high potency and selectivity to mu Opioid receptors. Dermorph ...
* DPDPE&nbs

*
Frakefamide Frakefamide (INN) is a synthetic, fluorinated linear tetrapeptide with the amino acid sequence Tyr-D-Ala-(''p''-F)Phe-Phe-NH2 which acts as a peripherally-specific, selective μ-opioid receptor agonist. Despite its inability to penetrate the ...
*
Gliadorphin Gliadorphin (also known as gluteomorphin) is an opioid peptide that is formed during digestion of the gliadin component of the gluten protein. It is usually broken down into amino acids by digestion enzymes. It has been hypothesized that children ...
*
Gluten exorphin Gluten exorphins are a group of opioid peptides formed during the digestion of the gluten Gluten is a structural protein naturally found in certain cereal grains. Although "gluten" often only refers to wheat proteins, in medical literature it r ...
s *
Hemorphin-4 Hemorphin-4 is an endogenous opioid peptide of the hemorphin family which possesses antinociceptive properties and is derived from the β-chain of hemoglobin in the bloodstream. It is a tetrapeptide with the amino acid sequence Tyr-Pro-Trp-Thr. ...
* Metkefamide *
Morphiceptin Morphiceptin is a tetrapeptide (Tyr-Pro-Phe-Pro-NH2) that is a selective μ-opioid receptor agonist. It is derived from β-casomorphin and has over 1,000 times selectivity for μ- over δ-opioid receptors. When injected intracerebroventricular ...
* Nociceptin *
Octreotide Octreotide, sold under the brand name Sandostatin among others, is an octapeptide that mimics natural somatostatin pharmacologically, though it is a more potent inhibitor of growth hormone, glucagon, and insulin than the natural hormone. It was ...
*
Opiorphin Opiorphin is an endogenous chemical compound first isolated from human saliva. Initial research with mice shows the compound has a painkilling effect greater than that of morphine. It works by stopping the normal breakup of enkephalins, natural ...
*
Rubiscolin The rubiscolins are a group of opioid peptides that are formed during digestion of the ribulose bisphosphate carboxylase/oxygenase (Rubisco) protein from spinach leaves. These peptides have much in common with the better-known gluten exorphin Glu ...
* Soymorphins * Spinorphin *
TRIMU 5 TRIMU-5 is a selective agonist of the μ2-opioid receptor and antagonist of the μ1-opioid receptor. It produces analgesia in animals that differs from that of conventional μ-opioid receptor agonists but that can still be blocked by μ-opioi ...
* Tynorphin *
Valorphin Valorphin, also known as VV-hemorphin-5, is a naturally occurring, endogenous opioid heptapeptide of the hemorphin family with the amino acid sequence H-Val-Val-Tyr-Pro-Trp-Thr-Gln-OH (VVYPWTQ). It is produced in the body via proteolyic cleavag ...
* Zyklophin


Others

* 3-(3-Methoxyphenyl)-3-ethoxycarbonyltropane  *
AD-1211 AD-1211 is an opioid analgesic drug invented in the 1970s by Dainippon Pharmaceutical Co. It is chemically a 1-substituted-4-prenyl-piperazine derivative, which is structurally unrelated to most other opioid drugs. The (''S'')-enantiomers in this ...
*
AH-7921 AH-7921 is an opioid analgesic drug selective for the μ-opioid receptor, having around 90% the potency of morphine when administered orally. It was discovered in the 1970s by a team at Allen and Hanburys located in the United Kingdom. The drug i ...
* Axomadol *
Azaprocin Azaprocin is a drug which is an opioid analgesic with approximately ten times the potency of morphine, and a fast onset and short duration of action. It was discovered in 1963, but has never been marketed. The derivative substituted on the pheny ...
*
BDPC BDPC (systematic name 4-(4-bromophenyl)-4-(dimethylamino)-1-(2-phenylethyl)cyclohexanol; also known as bromadol) is a potent narcotic analgesic with a distinctive arylcyclohexylamine chemical structure. It was developed by Daniel Lednicer at Upj ...
* Bisnortilidine 

* BRL-52537 *
Bromadol BDPC (systematic name 4-(4-bromophenyl)-4-(dimethylamino)-1-(2-phenylethyl)cyclohexanol; also known as bromadol) is a potent narcotic analgesic with a distinctive arylcyclohexylamine chemical structure. It was developed by Daniel Lednicer at Upj ...
* Bromadoline *
Ciprefadol Ciprefadol is an opioid analgesic that is an isoquinoline derivative most closely related to cyclazocine and picenadol, with a number of other related compounds known. Ciprefadol is a mixed agonist–antagonist at μ-opioid receptors and can p ...
* Ciramadol * Doxpicomine *
Enadoline Enadoline is a drug which acts as a highly selective kappa opioid receptor, κ-opioid agonist. In human studies, it produced visual distortions and feelings of dissociation (psychology), dissociation, reminiscent of the effects of salvinorin A. ...
*
Faxeladol Faxeladol (INN, USAN) (code names GRTA-9906, GRTA-0009906, EM-906, GCR-9905, GRT-TA300) is an opioid analgesic which was developed by Grünenthal GmbH but was never marketed for medical use anywhere in the world. It is related to tramadol and c ...
* GR-89696 * Herkinorin * ICI-199,441 *
ICI-204,448 ICI-204,448 is a drug which acts as a potent and peripherally selective κ-opioid agonist, with possible uses in the treatment of heart attack as well as anti-itching Itch (also known as pruritus) is a Wikt:sensation, sensation that causes ...
*
Ketamine Ketamine is a dissociative anesthetic used medically for induction and maintenance of anesthesia. It is also used as a recreational drug. It is one of the safest anesthetics, as, in contrast with opiates, ether, and propofol, it suppresses ne ...
* KNT-42 * LPK-26 * Lufuradom * Metofoline *
MT-45 MT-45 (IC-6) is an opioid analgesic drug invented in the 1970s by Dainippon Pharmaceutical Co. It is chemically a 1-substituted-4-(1,2-diphenylethyl)piperazine derivative, which is structurally unrelated to most other opioid drugs. Racemic MT-45 ...
* Desmethylclozapine * Nexeridine *
NNC 63-0532 NNC 63-0532 is a nociceptoid drug used in scientific research. It acts as a potent and selective agonist for the nociceptin receptor, also known as the ORL-1 ( opiate receptor-like 1) receptor. The function of this receptor is still poorly unde ...
*
Nortilidine Nortilidine is the major active metabolite of tilidine. It is formed from tilidine by demethylation in the liver. The racemate has opioid analgesic effects roughly equivalent in potency to that of morphine. The (1R,2S) isomer has NMDA antagonist ...
*
O-Desmethyltramadol Desmetramadol (), also known as ''O''-desmethyltramadol (''O''-DSMT), is an opioid analgesic and the main active metabolite of tramadol. Tramadol is demethylated by the liver enzyme CYP2D6 in the same way as codeine, and so similarly to the varia ...
* Phenadone *
Phencyclidine Phencyclidine or phenylcyclohexyl piperidine (PCP), also known as angel dust among other names, is a dissociative anesthetic mainly used recreationally for its significant mind-altering effects. PCP may cause hallucinations, distorted perceptio ...
* Prodilidine *
Profadol Profadol (CI-572) is an opioid analgesic which was developed in the 1960s by Parke-Davis. It acts as a mixed agonist-antagonist of the μ-opioid receptor. The analgetic potency is about the same as of pethidine (meperidine), the antagonistic eff ...
* Ro64-6198 *
Salvinorin A Salvinorin A is the main active psychotropic molecule in '' Salvia divinorum''. Salvinorin A is considered a dissociative hallucinogen. It is structurally distinct from other naturally occurring hallucinogens (such as DMT, psilocybin, and ...
*
Salvinorin B ethoxymethyl ether Salvinorin B methoxymethyl ether (2-''O''-methoxymethylsalvinorin B) is a semi-synthetic analogue of the natural product salvinorin A used in scientific research. It has a longer duration of action of around 2–3 hours, compared to less than 30 ...
* Salvinorin B methoxymethyl ether *
SB-612,111 SB-612,111 is an opioid receptor ligand which is a potent and selective antagonist for the nociceptin receptor (ORL-1), several times more potent than the older drug J-113,397. It does not have analgesic effects in its own right, but prevents th ...
* SC-17599 * RWJ-394,674 *
TAN-67 TAN-67 (SB-205,607) is an opioid drug used in scientific research that acts as a potent and selective delta opioid receptor, δ-opioid agonist, selective for the δ1 subtype. It has analgesic properties and induces dopamine release in nucleus acc ...
*
Tapentadol Tapentadol, brand names Nucynta among others, is a centrally acting opioid analgesic of the benzenoid class with a dual mode of action as an agonist of the μ-opioid receptor and as a norepinephrine reuptake inhibitor (NRI). Analgesia occurs wit ...
* Thiobromadol (C-8813) * Tifluadom * Tilidine *
Tramadol Tramadol, sold under the brand name Ultram among others, is an opioid pain medication used to treat moderate to moderately severe pain. When taken by mouth in an immediate-release formulation, the onset of pain relief usually begins within an h ...
*
Trimebutine Trimebutine is a drug with antimuscarinic and weak mu opioid agonist effects. It is used for the treatment of irritable bowel syndrome and other gastrointestinal disorders. The major product from drug metabolism of trimebutine in human beings ...
*
U-47700 U-47700, also known as U4, pink heroin, pinky, and pink, is an opioid analgesic drug developed by a team at Upjohn in the 1970s which has around 7.5 times the potency of morphine in animal models. U-47700 is a structural isomer of the earlier o ...
*
U-50,488 U-50488 is a drug which acts as a highly selective κ-opioid agonist, but without any μ-opioid antagonist effects. It has analgesic, diuretic and antitussive effects, and reverses the memory impairment produced by anticholinergic drugs. U-5 ...
*
U-69,593 U-69,593 is a drug which acts as a potent and selective κ1-opioid receptor agonist. In animal studies it has been shown to produce antinociception, anti-inflammation, anxiolysis (at low doses), respiratory depression, and diuresis, while ...
*
Viminol Viminol (marketed under the brandname Dividol) is an opioid analgesic developed by a team at the drug company Zambon in the 1960s. Viminol is based on the α-pyrryl-2-aminoethanol structure, unlike any other class of opioids. Viminol has both a ...
*
1-(4-Nitrophenylethyl)piperidylidene-2-(4-chlorophenyl)sulfonamide W-18 is a compound in a series of 32 substances (named W-1 to W-32) that were first synthesized in academic research on analgesic drug discovery in the 1980s and appeared as a designer drug in the 2010s. W-18 was invented at the University of A ...
(W-18)


Opioid

antagonists An antagonist is a character in a story who is presented as the chief foe of the protagonist. Etymology The English word antagonist comes from the Greek ἀνταγωνιστής – ''antagonistēs'', "opponent, competitor, villain, enemy, riv ...
and
inverse agonist In pharmacology, an inverse agonist is a drug that binds to the same receptor as an agonist but induces a pharmacological response opposite to that of the agonist. A neutral antagonist has no activity in the absence of an agonist or inverse agon ...
s

* 4-Caffeoyl-1,5-quinide * 5'-Guanidinonaltrindole * β-Funaltrexamine *
6β-Naltrexol 6β-Naltrexol, or 6β-hydroxynaltrexone (developmental code name AIKO-150), is a peripherally-selective opioid receptor antagonist related to naltrexone. It is a major active metabolite of naltrexone formed by hepatic dihydrodiol dehydrogenase ...
*
6β-Naltrexol-d4 6β-Naltrexol-d4, also known as 6β-hydroxynaltrexone-d4, is a deuterium-labeled form of 6β-naltrexol used for NMR imaging. Unlike opioid inverse agonists such as naloxone and naltrexone (which are often dubbed "antagonists" for simplicity's sa ...
*
Alvimopan Alvimopan (trade name Entereg) is a drug which behaves as a peripherally acting μ-opioid receptor antagonist. With the limited ability to cross the blood–brain barrier and reach the μ-opioid receptors of the central nervous system, the clin ...
* AT-076 * Binaltorphimine * BU09059 *
Buprenorphine Buprenorphine is an opioid used to treat opioid use disorder, acute pain, and chronic pain. It can be used under the tongue (sublingual), in the cheek (buccal), by injection (intravenous and subcutaneous), as a skin patch (transdermal), ...
*
Chlornaltrexamine Chlornaltrexamine is an irreversible mixed agonist–antagonist for μ-opioid receptors, which forms a covalent bond to the active site. It is 22 times more potent than morphine. Its alkylating group is a bis(chloroalkyl)amino-residue similar to ...
* Clocinnamox *
Cyclazocine Cyclazocine is a mixed opioid agonist/antagonist related to dezocine, pentazocine and phenazocine. This family of opioid drugs is called the benzomorphans or benzazocines. It is a KOR agonist and MOR partial agonist, and also has high affinity ...
*
Cyprodime Cyprodime is an opioid antagonist from the morphinan family of drugs. Cyprodime is a selective opioid antagonist which blocks the μ-opioid receptor, but without affecting the δ-opioid or κ-opioid receptors. This makes it useful for scien ...
*
Diacetylnalorphine Diacetylnalorphine (BAN), also known as ''O''3,''O''6-diacetyl-''N''-allyl-normorphine, is an opioid drug described as an analgesic and antidote which was never marketed. It is the 3,6-diacetyl ester of nalorphine, and therefore the heroin analog ...
&nbs

*
Diprenorphine Diprenorphine (brand name Revivon; former developmental code name M5050), also known as diprenorfin, is a non-selective, high- affinity, weak partial agonist of the μ- (MOR), κ- (KOR), and δ-opioid receptor (DOR) (with equal affinity) which ...
 (M5050) *
Fedotozine Fedotozine (INN; JO 1196 for the (-) tartrate salt) is an opioid drug of the arylacetamide series which acts as a peripherally specific selective κ1-opioid receptor agonist with preference for the κ1A subtype. It was under investigation f ...
* ICI-174864 *
J-113,397 J-113,397 is an opioid drug which was the first compound found to be a highly selective antagonist for the nociceptin receptor, also known as the ORL-1 receptor. It is several hundred times selective for the ORL-1 receptor over other opioid rece ...
*
JDTic JDTic is a selective, long-acting ("inactivating") antagonist of the κ-opioid receptor (KOR). JDTic is a 4-phenylpiperidine derivative, distantly related structurally to analgesics such as pethidine and ketobemidone, and more closely to the ...
*
JTC-801 JTC-801 is an opioid analgesic drug used in scientific research. JTC-801 is a selective antagonist for the nociceptin receptor, also known as the ORL-1 receptor. This was the fourth opioid receptor to be discovered and is still the least unders ...
*
Levallorphan Levallorphan ( INN, BAN) (brand names Lorfan, Naloxifan, Naloxiphan), also known as levallorphan tartrate (USAN), is an opioid modulator of the morphinan family used as an opioid analgesic and opioid antagonist/antidote. It acts as an antagonist ...
* LY-2456302 * LY-255582 * Methocinnamox *
Methylnaltrexone Methylnaltrexone (MNTX, brand name Relistor), used in form of methylnaltrexone bromide (INN, USAN, BAN), is a medication that acts as a peripherally acting μ-opioid receptor antagonist that acts to reverse some of the side effects of opioid dr ...
* ML350 *
Naldemedine Naldemedine (brand name Symproic in the US and Rizmoic in the European Union) is a medication that is used for the treatment of opioid-induced constipation in adults with chronic non-cancer pain. It is a peripherally acting μ-opioid receptor ant ...
*
Nalfurafine Nalfurafine (INN, USAN) (brand name Remitch; former developmental code names TRK-820, AC-820, MT-9938) is an antipruritic (anti-itch drug) that is marketed in Japan for the treatment of uremic pruritus in individuals with chronic kidney disease u ...
*
Nalmefene Nalmefene is an opioid antagonist medication used in the management of opioid overdose and alcohol dependence. It is taken by mouth. Nalmefene is an opiate derivative similar in both structure and activity to the opioid antagonist naltrexone. ...
* Nalmexonebr>
*
Nalodeine Nalodeine, also known more commonly as N-allylnorcodeine, is an opioid antagonist (specifically, an antagonist of the μ-opioid receptor) that was never marketed but is notable as the first opioid antagonist to be discovered. It was first reporte ...
 (N-allylnorcodeine)&nbs

*
Naloxazone Naloxazone is an irreversible μ-opioid receptor antagonist which is selective for the μ1 receptor subtype. Naloxazone produces very long lasting antagonist effects as it forms a covalent bond to the active site of the μ-opioid receptor, thu ...
*
Naloxegol Naloxegol (INN; PEGylated naloxol; trade names Movantik and Moventig) is a peripherally acting μ-opioid receptor antagonist developed by AstraZeneca, licensed from Nektar Therapeutics, for the treatment of opioid-induced constipation. It was app ...
*
Naloxol Naloxol is an opioid antagonist closely related to naloxone. It exists in two isomeric forms, α-naloxol and β-naloxol. α-naloxol is a human metabolite of naloxone. Synthetically, α-naloxol can be prepared from naloxone by reduction of the ...
*
Naloxonazine Naloxonazine is a potent, irreversible μ-opioid receptor The μ-opioid receptors (MOR) are a class of opioid receptors with a high affinity for enkephalins and beta-endorphin, but a low affinity for dynorphins. They are also referred to as ...
*
Naloxone Naloxone, sold under the brand names Narcan (4 mg) and Kloxxado (8 mg) among others, is a medication used to reverse or reduce the effects of opioids. It is commonly used to counter decreased breathing in opioid overdose. Effects begin within ...
* Naloxone benzoylhydrazone *
Nalorphine Nalorphine () (brand names Lethidrone, Nalline), also known as ''N''-allylnormorphine, is a mixed opioid agonist–antagonist with opioid antagonist and analgesic properties. It was introduced in 1954 and was used as an antidote to reverse op ...
*
Naltrexone Naltrexone, sold under the brand name Revia among others, is a medication primarily used to manage alcohol or opioid use disorder by reducing cravings and feelings of euphoria associated with substance use disorder. It has also been found t ...
* Naltriben *
Naltrindole Naltrindole is a highly potent, highly selective delta opioid receptor antagonist used in biomedical research. In May 2012 a paper was published in ''Nature'' with the structure of naltrindole in complex with the mouse δ-opioid G-protein coupled ...
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Norbinaltorphimine Norbinaltorphimine (nor-BNI or nBNI) is an opioid antagonist used in scientific research. It is one of the few opioid antagonists available that is highly selective for the κ-opioid receptor, and blocks this receptor without affecting the μ- ...
* Oxilorphan *
PF-4455242 PF-4455242 is a selective, short-acting (non-"inactivating") antagonist of the κ-opioid receptor. Discovered by Pfizer Pfizer Inc. ( ) is an American multinational pharmaceutical and biotechnology corporation headquartered on 42nd Stree ...
* S-allyl-3-hydroxy-17-thioniamorphinan (SAHT

*
Samidorphan Samidorphan (, ) (developmental code names ALKS-33, RDC-0313), is an opioid antagonist which in the form of olanzapine/samidorphan (brand name Lybalvi) is used in the treatment of schizophrenia and bipolar disorder. Samidorphan reduces the weight ...
  * SR-16430


Biased ligands Bias is an inclination toward something, or a predisposition, partiality, prejudice, preference, or predilection. Bias may also refer to: Scientific method and statistics * The bias introduced into an experiment through a confounder * Algo ...

* 6'-Guanidinonaltrindole *
7-Hydroxymitragynine 7-Hydroxymitragynine is a terpenoid indole alkaloid from the plant ''Mitragyna speciosa'', commonly known as Kratom. It is often referred to as ‘7-OH’. It was first described in 1994 and is a natural product derived from the mitragynine prese ...
* Herkinorin * ICI-199,441 *
Noribogaine Noribogaine (actually O-desmethylibogaine), or 12-hydroxyibogamine, is the principal psychoactive metabolite of the oneirogen ibogaine. It is thought to be involved in the antiaddictive effects of ibogaine-containing plant extracts, such as '' ...
*
Oliceridine Oliceridine, sold under the brand name Olinvyk, is an opioid medication that is used for the treatment of moderate to severe acute pain in adults. It is given by intravenous (IV) injection. The most common side effects include nausea, vomiting, ...
*
RB-64 RB-64 (22-thiocyanatosalvinorin A) is a semi-synthetic salvinorin A, salvinorin derivative and a κ-opioid receptor (KOR) agonist which is used in scientific research. Its most remarkable property is its functional selectivity for G protein versu ...
*
TRV734 TRV734 is a drug developed by Trevena Inc which acts as a biased agonist at the μ-opioid receptor, selective for activation of the G-protein signalling pathway over β-arrestin 2 recruitment. It is closely related to oliceridine Oliceridine ...


Receptor heteromer targeting ligands

* 6'-GNTI (δ-κ) * CYM-51010 (δ-μ) * NNTA (κ-μ) * IBNtxA (μ1G-NOP)


Uncategorized opioids

* ADL-5859 * Alimadol *
Amentoflavone Amentoflavone is a biflavonoid (''bis''-apigenin coupled at 8 and 3' positions, or 3′,8′′-biapigenin) constituent of a number of plants including ''Ginkgo biloba'', ''Chamaecyparis obtusa'' (hinoki), '' Hypericum perforatum'' (St ...
* Anilopambr>+HCl
*
Asimadoline Asimadoline (EMD-61753) is an experimental drug which acts as a peripherally selective κ-opioid receptor (KOR) agonist. Because of its low penetration across the blood–brain barrier, asimadoline lacks the psychotomimetic effects of centrally ...
*
Cyproterone acetate Cyproterone acetate (CPA), sold alone under the brand name Androcur or Ethinylestradiol/cyproterone acetate, with ethinylestradiol under the brand names Diane or Diane-35 among others, is an antiandrogen and progestin medication used in the treat ...
* FE 200665 *
Fedotozine Fedotozine (INN; JO 1196 for the (-) tartrate salt) is an opioid drug of the arylacetamide series which acts as a peripherally specific selective κ1-opioid receptor agonist with preference for the κ1A subtype. It was under investigation f ...
* HZ-2 *
Kolokol-1 Kolokol-1 (russian: Колокол meaning "bell") is a synthetic opioid developed for use as an aerosolizable incapacitating agent. The exact chemical structure has not yet been revealed by the Russian government. It was originally thought by so ...
* Matrine * MCOPPB *
Menthol Menthol is an organic compound, more specifically a monoterpenoid, made synthetically or obtained from the oils of corn mint, peppermint, or other mints. It is a waxy, clear or white crystalline substance, which is solid at room temperature and ...
* MT-7716 *
Nalfurafine Nalfurafine (INN, USAN) (brand name Remitch; former developmental code names TRK-820, AC-820, MT-9938) is an antipruritic (anti-itch drug) that is marketed in Japan for the treatment of uremic pruritus in individuals with chronic kidney disease u ...
*
Nalorphine Nalorphine () (brand names Lethidrone, Nalline), also known as ''N''-allylnormorphine, is a mixed opioid agonist–antagonist with opioid antagonist and analgesic properties. It was introduced in 1954 and was used as an antidote to reverse op ...
*
Nalorphine dinicotinate Nalorphine dinicotinate (trade name Nimelan), also known as ''N''-allylnormorphine dinicotinate, dinicotinoylnalorphine, or niconalorphine, is a semisynthetic, mixed opioid agonist- antagonist which is described as a narcotic antagonist but may ...
*
PZM21 PZM21 is an experimental opioid analgesic drug that is being researched for the treatment of pain. It is claimed to be a functionally selective μ-opioid receptor agonist which produces μ-opioid receptor mediated G protein signaling, with potenc ...
*
Proglumide Proglumide (Milid) is a drug that inhibits gastrointestinal motility and reduces gastric secretions. It acts as a cholecystokinin antagonist, which blocks both the CCKA and CCKB subtypes. It was used mainly in the treatment of stomach ulcers, ...
* Ro65-6570  * SoRI-9409  *
Spiradoline Spiradoline (U-62066) is a drug which acts as a highly selective κ-opioid agonist. It has analgesic, diuretic, and antitussive effects, and produces subjective effects in animals similar to those of ketazocine and alazocine. The main effect ...
  * SR-8993  *
SR-16435 SR-16435 is a drug which acts as a potent partial agonist at both the μ-opioid receptor and nociceptin receptor. In animal studies it was found to be a potent analgesic, with results suggestive of reduced development of tolerance and increased a ...


Combination drug formulations containing opioids

* Buprenorphine/naloxone * Buprenorphine/samidorphan (ALKS-5461) *
Co-codamol Codeine/paracetamol, also known as codeine/acetaminophen and co-codamol, is a compound analgesic consisting of a combination of codeine phosphate and paracetamol (acetaminophen). Codeine/paracetamol is used for the relief of mild to moderate pai ...
(codeine phosphate/paracetamol) *
Co-codaprin Co-codaprin ( BAN) is a non-proprietary name used to denote a compound analgesic, a combination of codeine phosphate with aspirin. Co-codaprin tablets are used for mild to moderate pain. Preparations Canada AC&C is a preparation of aspirin, c ...
(codeine phosphate/aspirin) *
Co-dydramol Co-dydramol ( BAN) is a non-proprietary name used to denote a particular compound analgesic, a combination of dihydrocodeine tartrate and paracetamol. Co-dydramol tablets are used for the relief of moderate pain. Co-dydramol is part of a seri ...
(dihydrocodeine tartrate/paracetamol) *
Co-proxamol Dextropropoxyphene is an analgesic in the opioid category, patented in 1955 and manufactured by Eli Lilly and Company. It is an optical isomer of levopropoxyphene. It is intended to treat mild pain and also has antitussive (cough suppressant) a ...
(dextropropoxyphene/paracetamol) * Fentanyl/fluanisone *
Hydrocodone/ibuprofen Hydrocodone/ibuprofen (INNs), sold under the brand name Vicoprofen, is a fixed-dose combination analgesic medication used in short-term therapy to relieve severe pain. Vicoprofen combines the analgesic and antitussive properties of hydrocodone ...
*
Hydrocodone/paracetamol Hydrocodone/paracetamol (also known as hydrocodone/acetaminophen) is the combination of the pain medications hydrocodone and paracetamol (acetaminophen). It is used to treat moderate to severe pain. It is taken by mouth. Recreational use is co ...
* Loperamide/simethicone * Morphine/naltrexone *
Naltrexone/bupropion Naltrexone/bupropion, sold under the brand name Contrave among others, is a fixed-dose combination medication for the management of chronic obesity in adults in combination with a reduced-calorie diet and increased physical activity. It contains ...
*
Oxycodone/aspirin Oxycodone/aspirin (trade name Percodan) is a combination drug marketed by Endo Pharmaceuticals. It is a tablet containing a mixture of 325 mg (5 Grain (unit), grains) of aspirin and 4.8355 mg of oxycodone, oxycodone HCl (equivalent to ...
*
Oxycodone/naloxone Oxycodone/naloxone, sold under the trade name Targin and Targinact (in the UK) among others, is a combination pain medication. It is available as modified-release tablets and is taken by mouth. The oxycodone component is an opioid and is respon ...
*
Oxycodone/paracetamol Oxycodone/paracetamol, sold under the brand name Percocet among others, is a fixed-dose combination of the opioid oxycodone with paracetamol (acetaminophen), used to treat moderate to severe pain. In 2020, it was the 69th most commonly prescri ...


See also

* List of opioids by visual 2D molecular skeletal renderings (bundled remotely, click "show" after following link) *
List of Schedule I drugs (US) This is the list of Schedule I drugs as defined by the United States Controlled Substances Act. 21 CFRbr>1308.11(CSA Sched I) with changes through (Oct 18, 2012). Retrieved September 6, 2013. The following findings are required for drugs to be pla ...
* Gray death


References


External links


Carbonate derivatives of 14β-hydroxycodeine
"''viz''., 14β-hydroxy-6-''O''-(methoxycarbonyl)codeine, 6-''O''-methoxycarbonyl-14β-(methoxycarbonyloxy)codeine, and 14β-acetoxy-6-''O''-methoxy-carbonylcodeine, potential substrates for ring ''C'' modification in morphinane (''sic'') alkaloids, were synthesized for the first time." ''Russian Chemical Bulletin.'' August 2008, Volume 57, Issue 8, pp 1773–1774. Date: 11 Aug 2009; I. V. Evsikova, S. K. Moiseev, P. V. Petrovskii, V. N. Kalinin. Published in Russian in ''Izvestiya Akademii Nauk. Seriya Khimicheskaya'', No. 8, pp. 1739–1740 {{Opioidergics *List
Opioids Opioids are substances that act on opioid receptors to produce morphine-like effects. Medically they are primarily used for pain relief, including anesthesia. Other medical uses include suppression of diarrhea, replacement therapy for opioid use ...