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Acetoxymethylketobemidone
Acetoxymethylketobemidone (O-AMKD), is an opioid designer drug related to ketobemidone, with around the same potency as morphine. It was first identified in Germany in October 2020. See also * 2F-Viminol * 3-HO-PCP * 4-Fluoropethidine * Acetoxyketobemidone * Bucinnazine * Dipyanone * Etodesnitazene * Methylketobemidone * Nortilidine * O-Desmethyltramadol * Piperidylthiambutene * 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 ... References Synthetic opioids 4-Phenylpiperidines Mu-opioid receptor agonists {{analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 metabolite norketobemidone. This may make it useful for some types of pain that do not respond well to other opioids. It is marketed in Denmark, Iceland, Norway and Sweden and is used for severe pain. History Ketobemidone was first synthesized in 1942 by Eisleb and colleagues, at the laboratory of I.G. Farbenindustrie at Hoechst during the Second World War. The first study of it in humans was published in 1946, and it was introduced in clinical medicine shortly after. It was not in clinical use in the United States when the Controlled Substances Act 1970 was promulgated and was assigned to Schedule I with an ACSCN of 9628. As of 2013, no annual manufacturing quota was assigned by the DEA. Pfizer manufactures ketobemidone under the trad ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 use disorder, reversing opioid overdose, and suppressing cough. Extremely potent opioids such as carfentanil are approved only for veterinary use. Opioids are also frequently used non-medically for their euphoric effects or to prevent withdrawal. Opioids can cause death and have been used for executions in the United States. Side effects of opioids may include itchiness, sedation, nausea, respiratory depression, constipation, and euphoria. Long-term use can cause tolerance, meaning that increased doses are required to achieve the same effect, and physical dependence, meaning that abruptly discontinuing the drug leads to unpleasant withdrawal symptoms. The euphoria attracts recreational use, and frequent, escalating recreational use of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Etodesnitazene
Etodesnitazene (Desnitroetonitazene, Etazen, Etazene, Etazone) is a benzimidazole derived opioid analgesic drug, which was originally developed in the late 1950s alongside etonitazene and a range of related derivatives. It is many times less potent than etonitazene itself, but still 70x more potent than morphine in animal studies. Corresponding analogues where the N,N-diethyl group is replaced by piperidine or pyrrolidine rings also retain significant activity (10x and 20x morphine respectively). Etodesnitazene has been sold as a designer drug, first being identified in both Poland and Finland in March 2020. See also * Brorphine * Etonitazepyne * Isotonitazene * Metonitazene * Metodesnitazene * MCHB-1 * List of benzimidazole opioids Benzimidazole opioids, also known as nitazenes, are a class of synthetic opioids with an unusual benzimidazole structure often referred to as opioid New Psychoactive Substances (opioid NPS). First synthesized in the 1950s by CIBA Pharmaceuticals ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Synthetic 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 disorder, reversing opioid overdose, and suppressing cough. Extremely potent opioids such as carfentanil are approved only for veterinary use. Opioids are also frequently used non-medically for their euphoric effects or to prevent withdrawal. Opioids can cause death and have been used for executions in the United States. Side effects of opioids may include itchiness, sedation, nausea, respiratory depression, constipation, and euphoria. Long-term use can cause tolerance, meaning that increased doses are required to achieve the same effect, and physical dependence, meaning that abruptly discontinuing the drug leads to unpleasant withdrawal symptoms. The euphoria attracts recreational use, and frequent, escalating recreational use of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 list of drugs under international control, probably because it was not used in medicine or widely available. Propylketobemidone is so named because it is the propyl ketone analogue of bemidone (hydroxypethidine). The more commonly used ethyl ketone ("ethylketobemidone") is simply called ketobemidone, as it is the only drug of this family to have been marketed. Presumably propylketobemidone produces similar effects to ketobemidone and other opioids, such as analgesia and sedation, along with side effects such as nausea, itching, vomiting and respiratory depression Hypoventilation (also known as respiratory depression) occurs when ventilation is inadequate (''hypo'' meaning "below") to perform needed respiratory gas exchange. By def ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 synthetic opioids previously reported. If sold or obtained for the purpose of human consumption it could be considered a controlled substance analogue in some countries such as the US, Australia and New Zealand. Piperidylthiambutene has been sold as a 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. D ..., first appearing in late 2018. Synthesis The Grignard reaction between 3-Piperidinobutyric acid ethyl esterCID:10774378(1) and 2-Bromothiophene 003-09-4(2) gives 3. Dehydration in acid completes the synthesis. References Opioi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 variation in effects seen with codeine, individuals who have a less active form of CYP2D6 ("poor metabolizers") will tend to get reduced analgesic effects from tramadol. This also results in a ceiling effect (dependent on CYP2D6 availability) which limits tramadol's range of therapeutic benefits to the treatment of moderate pain. Pharmacology Pharmacodynamics (+)-Desmetramadol is a G-protein biased μ-opioid receptor full agonist. It shows comparatively far lower affinity for the δ- and κ-opioid receptors. The two enantiomers of desmetramadol show quite distinct pharmacological profiles; both (+) and (−)-desmetramadol are inactive as serotonin reuptake inhibitors, but (−)-desmetramadol retains activity as a norepinephrine reuptake inhi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 activity. The drug also acts as a dopamine reuptake inhibitor. The reversed-ester of nortilidine is also known, as is the corresponding analogue with the cyclohexene ring replaced by cyclopentane, which have almost identical properties to nortilidine. Use Nortilidine has been sold as a designer drug, first being identified in Poland in May 2020. See also * Desmetramadol, another opioid metabolite with additional (non-opioid) mechanisms of analgesia, which has also been sold as a designer drug * 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). Analges ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 list of drugs under international control, probably because it was not used in medicine or widely available. Methylketobemidone is so named because it is the methyl ketone analogue of bemidone (hydroxypethidine). The more commonly used ethyl ketone ("ethylketobemidone") is simply called ketobemidone, as it is the only drug of this family to have been marketed. Presumably methylketobemidone produces similar effects to ketobemidone and other opioids, such as analgesia and sedation, along with side effects such as nausea, itching, vomiting and respiratory depression Hypoventilation (also known as respiratory depression) occurs when ventilation is inadequate (''hypo'' meaning "below") to perform needed respiratory gas exchange. By def ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dipyanone
Dipyanone is an opioid analgesic which has been sold as a designer drug, first identified in Germany in 2021. It is closely related to medically used drugs such as methadone, dipipanone and phenadoxone, but is slightly less potent. See also * Desmethylmoramide * IC-26 * Nufenoxole * 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 ... References Opioids Pyrrolidines Mu-opioid receptor agonists Ketones {{analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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. Designer drugs include psychoactive substances that have been designated by the European Union as new psychoactive substances (NPS) as well as analogs of performance-enhancing drugs such as designer steroids. Some of these were originally synthesized by academic or industrial researchers in an effort to discover more potent derivatives with fewer side effects, and shorter duration (and possibly also because it is easier to apply for patents for new molecules) and were later co-opted for recreational use. Other designer drugs were prepared for the first time in clandestine laboratories. Because the efficacy and safety of these substances have not been thoroughly evaluated in animal and human trials, the use of some of these drugs may result i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bucinnazine
Bucinnazine (AP-237, 1-butyryl-4-cinnamylpiperazine) is an opioid analgesic drug that was widely used in China to treat pain in cancer patients as of 1986. It is one of the most potent compounds among a series of piperazine-amides first synthesized and reported in Japan in the 1970s. Bucinnazine has analgesic potency comparable to that of morphine but with a relatively higher therapeutic index. The drug was initially claimed to be a non-narcotic analgesic. However, subsequent studies have shown bucinnazine and similar acyl piperazines to be potent and selective agonists of μ-opioid receptor (MOR) with relatively low affinity for the δ-opioid receptor and the κ-opioid receptor. In accordance with these studies, results from the intravenous self-administration experiments in rats showed that bucinnazine has a marked reinforcing effect with tolerance and dependence quickly developing. In addition, the morphine antagonist naloxone reverses the effect of bucinnazine and precip ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
