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PEPAP
PEPAP (phenethylphenylacetoxypiperidine) is an opioid analgesic that is an analog of desmethylprodine. It is related to the drug MPPP, with an ''N''-phenethyl group in place of the ''N''-methyl substitution and an acetate ester rather than propionate. PEPAP is approximately 6–7 times more potent than morphine in laboratory rats. PEPAP presumably has similar effects to other opioids, producing analgesia, sedation and euphoria. Side effects can include itching, nausea and potentially serious respiratory depression which can be life-threatening. PEPAP has been found to be a potent CYP2D6 inhibitor, which makes it likely to cause adverse interactions with some other drugs, although the inhibitory potency of PEPAP is less than that of MPPP. Both cocaine and methadone are also CYP2D6 inhibitors and could, in theory, potentiate the effect. It is unlikely that the tetrahydropyridine byproducts that may be formed during the synthesis of PEPAP are neurotoxic in the same way as th ...
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Opioid
Opioids are a class of Drug, drugs that derive from, or mimic, natural substances found in the Papaver somniferum, opium poppy plant. Opioids work on opioid receptors in the brain and other organs to produce a variety of morphine-like effects, including analgesic, pain relief. The terms "opioid" and "opiate" are sometimes used interchangeably, but the term "opioid" is used to designate all substances, both natural and synthetic, that bind to opioid receptors in the brain. Opiates are alkaloid compounds naturally found in the opium poppy plant ''Papaver somniferum''. Medically they are primarily used for pain relief, including anesthesia. Other medical uses include suppression of diarrhea, replacement therapy for opioid use disorder, and Cold medicine, suppressing cough. The opioid receptor antagonist naloxone is used to reverse opioid overdose. Extremely potent opioids such as carfentanil are approved only for Veterinary medicine, veterinary use. Opioids are also frequently use ...
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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 DEA as a Schedule I drug in the United States. It is an analog of pethidine (meperidine) a Schedule II drug. Chemically, it is a reversed ester of pethidine which has about 70% of the potency of morphine. Unlike its derivative prodine, it does not exhibit optical isomerism. It was reported to have 30 times the activity of pethidine and a greater analgesic effect than morphine in rats, and it was demonstrated to cause central nervous system stimulation in mice. History Desmethylprodine was first synthesized in 1947 at Hoffman-LaRoche Laboratories by Albert Ziering and John Lee. They found that it produced effects similar to morphine when administered to rats. Ziering had been searching for synthetic painkillers that were less addictive than morphine. The new drug was a slig ...
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Pheneridine
Pheneridine is a 4-phenylpiperidine derivative that is related to the opioid analgesic drug pethidine (meperidine). Pheneridine is not currently used in medicine. Presumably it has similar effects to other opioid derivatives, such as analgesia, sedation, nausea and respiratory depression, however unlike most opioid derivatives it is not specifically listed as an illegal drug, although it would probably be regarded as a controlled substance analogue of pethidine on the grounds of its related chemical structure in some jurisdictions such as the United States, Canada and Australia, and would be classified as a "Pethidine Analogue" under the New Zealand Misuse of Drugs Act Class C7. See also *Anileridine *PEPAP *Diphenoxylate *Pethidine Pethidine, also known as meperidine and sold under the brand name Demerol among others, is a fully synthetic opioid pain medication of the phenylpiperidine class. Synthesized in 1938 as a potential anticholinergic agent by the German chemist Ot ...
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LS-115509
LS-115509 is an opioid analgesic related to the 4-phenylpiperidine family. It is comparable to drugs such as prodine and pheneridine, but is distinguished by the presence of an ether group and furan ring at the piperidine 4-position, which are not found in other drugs of this class. In animal studies, it has around 2-3x the potency of morphine depending on what assay is used. Like prodine, it has two stereocenters and four possible enantiomers, but the activity of these has not been tested separately. See also * PEPAP PEPAP (phenethylphenylacetoxypiperidine) is an opioid analgesic that is an analog of desmethylprodine. It is related to the drug MPPP, with an ''N''-phenethyl group in place of the ''N''-methyl substitution and an acetate ester rather than ... References Synthetic opioids Piperidines Ethers Mu-opioid receptor agonists 2-Furyl compounds Ethoxy compounds {{analgesic-stub ...
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OPPPP
OPPPP (1-(3-Oxo-3-phenylpropyl)-4-phenyl-4-piperidinyl propionate) is one of several compounds derived from MPPP, the reversed ester of the opioid analgesic pethidine, which were sold as designer drugs in the 1980s, but have been rarely encountered by law enforcement since the passage of the Federal Analogue Act in 1986. In animal studies it was found to be around 1000× the potency of pethidine, making it several times the potency of fentanyl and with similar hazards of respiratory depression and overdose. It is closely related to numerous compounds made by Janssen et al. for which the structure-activity relationship is well established. See also * List of fentanyl analogues * PEPAP * LY-88329 LY-88329 is an opioid receptor ligand related to medicines such as pethidine. It has high affinity to the μ-opioid receptor, but unlike structurally related drugs such as 3-methylfentanyl and OPPPP, LY-88329 is a potent opioid antagonist. In a ... References 4-Phenylpiperidin ...
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Neurotoxicity
Neurotoxicity is a form of toxicity in which a biological, chemical, or physical agent produces an adverse effect on the structure or function of the central and/or peripheral nervous system. It occurs when exposure to a substance – specifically, a neurotoxin or neurotoxicant– alters the normal activity of the nervous system in such a way as to cause permanent or reversible damage to nervous tissue. This can eventually disrupt or even kill neurons, which are cells that transmit and process signals in the brain and other parts of the nervous system. Neurotoxicity can result from organ transplants, radiation treatment, certain drug therapies, recreational drug use, exposure to heavy metals, bites from certain species of venomous snakes, pesticides, certain industrial cleaning solvents, fuels and certain naturally occurring substances. Symptoms may appear immediately after exposure or be delayed. They may include limb weakness or numbness, loss of memory, vision, and/or inte ...
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Acetate Esters
An acetate is a salt formed by the combination of acetic acid with a base (e.g. alkaline, earthy, metallic, nonmetallic, or radical base). "Acetate" also describes the conjugate base or ion (specifically, the negatively charged ion called an anion) typically found in aqueous solution and written with the chemical formula . The neutral molecules formed by the combination of the acetate ion and a ''positive'' ion (called a cation) are also commonly called "acetates" (hence, ''acetate of lead'', ''acetate of aluminium'', etc.). The simplest of these is hydrogen acetate (called acetic acid) with corresponding salts, esters, and the polyatomic anion , or . Most of the approximately 5 million tonnes of acetic acid produced annually in industry are used in the production of acetates, which usually take the form of polymers. In nature, acetate is the most common building block for biosynthesis. Nomenclature and common formula When part of a salt, the formula of the acetate ion is ...
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Phenethylamines
Substituted phenethylamines (or simply phenethylamines) are a chemical class of organic compounds that are based upon the phenethylamine structure; the class is composed of all the derivative (chemistry), derivative compounds of phenethylamine which can be formed by replacing, or substitution reaction, substituting, one or more hydrogen atoms in the phenethylamine core structure with substituents. Phenylethylamines are also generally found to be central nervous system stimulants with many also being entactogens/empathogens, and hallucinogens. Structural classification The structural formula of any substituted phenethylamine contains a phenyl group, phenyl ring that is joined to an amino group, amino (NH) group via a two-carbon substituent, sidechain. Hence, any substituted phenethylamine can be classified according to the substitution of hydrogen atom, hydrogen (H) atoms on phenethylamine's phenyl ring, sidechain, or amino group with a moiety (chemistry), specific group of at ...
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Fentanyl
Fentanyl is a highly potent synthetic piperidine opioid primarily used as an analgesic (pain medication). It is 30 to 50 times more Potency (pharmacology), potent than heroin and 50 to 100 times more potent than morphine. Its primary Medicine, clinical utility is in pain management for cancer patients and those recovering from painful surgeries. Fentanyl is also used as a sedative. Depending on the method of delivery, fentanyl can be very fast acting and ingesting a relatively small quantity can cause overdose. Fentanyl works by activating μ-opioid receptors. Fentanyl is sold under the brand names Actiq, Duragesic, and Sublimaze, among others. Pharmaceutical fentanyl's adverse effects are similar to those of other opioids and narcotics including addiction, confusion, hypoventilation, respiratory depression (which, if extensive and untreated, may lead to respiratory arrest), drowsiness, nausea, visual disturbances, dyskinesia, hallucinations, delirium, a subset of the latte ...
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