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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, which boosts affinity to the μ-opioid receptor, and so phenomorphan is around 10x more potent than levorphanol, which is itself 6-8x the potency of morphine. Other analogues where the N-(2-phenylethyl) group has been replaced by other aromatic rings are even more potent, with the N-(2-(2-furyl)ethyl) and the N-(2-(2-thienyl)ethyl) analogues being 60x and 45x stronger than levorphanol, respectively. See also * 14-Cinnamoyloxycodeinone * 14-Phenylpropoxymetopon * 7-PET * N-Phenethylnormorphine * N-Phenethylnordesomorphine * N-Phenethyl-14-ethoxymetopon * RAM-378 RAM-378(7,8-Dihydro-14-hydroxy-N-phenethylnormorphine) is an opioid analgesic. It is the N-phenethyl derivative of hydromorphinol Hydromorphinol (RAM-320, 14-hydroxydi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
14-Phenylpropoxymetopon
14-Phenylpropoxymetopon (PPOM) is an opioid 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, with an even higher ''in vivo'' potency than etorphine. The 14-phenylpropoxy substitution appears to confer potent μ-opioid agonist activity, even when combined with substitutions such as N-cyclopropyl or N-allyl, which normally result in μ-opioid antagonist compounds. It has never been used in humans, but would be expected to produce effects similar to those of other potent opioid agonists, including strong analgesia, sedation, euphoria, constipation, itching and respiratory depression which could be harmful or fatal. Tolerance and dependence would be expected to develop rapidly based on the potency of the drug, as it is of a similar strength to the most potent of fentanyl analogues and so would most likely cause pronounced tachyph ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Morphinans
Morphinan is the prototype chemical structure of a large chemical class of psychoactive drugs, consisting of opiate analgesics, cough suppressants, and dissociative drug, dissociative hallucinogens, among others. Typical examples include compounds such as morphine, codeine, and dextromethorphan (DXM). Despite related molecular structures, the pharmacological profiles and mechanisms of action between the various types of morphinan substances can vary substantially. They tend to function either as μ-opioid receptor agonists (analgesics), or NMDA receptor antagonists (dissociatives). Structure Morphinan has a phenanthrene core structure with the ''A'' ring remaining aromatic and the ''B'' and ''C'' rings being saturated, and an additional nitrogen-containing, six-membered, saturated ring, the ''D'' ring, being attached to carbons 9 and 13 of the core, and with the nitrogen being at position 17 of the composite. Of the major naturally occurring opiates of the morphinan type—morp ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
RAM-378
RAM-378(7,8-Dihydro-14-hydroxy-N-phenethylnormorphine) is an opioid analgesic. It is the N-phenethyl derivative of hydromorphinol Hydromorphinol (RAM-320, 14-hydroxydihydromorphine), 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, anal .... See also * 14-Cinnamoyloxycodeinone * 14-Phenylpropoxymetopon * 7-PET * N-Phenethylnormorphine * N-Phenethyl-14-ethoxymetopon * Phenomorphan * Ro4-1539 References 4,5-Epoxymorphinans Semisynthetic opioids {{Analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 both μ- and δ-opioid receptors, with a Ki of 0.16 nM at μ and 3.14 nM at δ. See also * 14-Cinnamoyloxycodeinone * 14-Phenylpropoxymetopon * 7-PET * MR-2096 * N-Phenethylnormorphine * Phenomorphan * RAM-378 RAM-378(7,8-Dihydro-14-hydroxy-N-phenethylnormorphine) is an opioid analgesic. It is the N-phenethyl derivative of hydromorphinol Hydromorphinol (RAM-320, 14-hydroxydihydromorphine), is an opiate analogue that is a derivative of morphine, wher ... * Ro4-1539 References Delta-opioid receptor agonists 4,5-Epoxymorphinans Hydroxyarenes Ketones Ethers Mu-opioid receptor agonists Semisynthetic opioids Ethoxy compounds {{analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 most other N-substituted derivatives of morphine, which are substantially less active, or act as antagonists. Binding studies have helped to explain the increased potency of N-phenethylnormorphine, showing that the phenethyl group extends out to reach an additional binding point deeper inside the μ-opioid receptor cleft, analogous to the binding of the phenethyl group on fentanyl. See also * 14-Cinnamoyloxycodeinone * 14-Phenylpropoxymetopon * 7-PET * MR-2096 * ''N''-Phenethyl-14-ethoxymetopon * ''N''-Phenethylnordesomorphine * Phenomorphan * RAM-378 RAM-378(7,8-Dihydro-14-hydroxy-N-phenethylnormorphine) is an opioid analgesic. It is the N-phenethyl derivative of hydromorphinol Hydromorphinol (RAM-320, 14-hydroxydihydromorphine ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 anesthetic medication for the sedation of large animals such as elephants, giraffes, and rhinos. 7-PET itself has a 3-''O''-methyl ether which reduces potency, but the 3-OH derivative is around 2200 times more potent than morphine, almost the same potency as etorphine as a μ agonist, and unexpectedly the 3-hydrogen compound is also around the same potency of 2000 times morphine. Unlike etorphine, 7-PET is not controlled under the UN drug conventions, but it might still be considered to be a controlled substance analogue of etorphine on the grounds of its related chemical structure in some jurisdictions such as the United States, Canada, Australia, and New Zealand. See also * 14-Cinnamoyloxycodeinone * 14-Phenylpropoxymetopon * BU72 * ''N''-P ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 times more potent than the related drug levorphanol in animal experiments. Although it has high potency, long duration, and good therapeutic index (1100 in animal studies),Bulletin on Narcotics October–December 1956 page 37 Ro4-1539 had no particular clinical advantages over other available opioid drugs, and was never commercially marketed. Ro4-1539 has never formally undergone clinical trials in humans, but based on its effects in animals it would be expected to produce effects similar to those of other potent opioid agonists, including strong analgesia, sedation, euphoria, constipation, itching, tachyphylaxis and respiratory depression, which could be harmful or fatal. Due to potential κ-opioid agonism, it may be somewhat dysphoric a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
14-Cinnamoyloxycodeinone
14-Cinnamoyloxycodeinone is the most potent example in a series of opiate analgesic drugs discovered in the 1960s, with over 100 times the potency of morphine. It is a derivative of , being the 14-cinnamate ester. In another paper, Buckett assigns the potency as 177 with a range (depending on animal and test) of 101–310×. It may be of interest to researchers that the allyl group in this compound and in allylprodine overlay very closely. See also * 14-Phenylpropoxymetopon * 7-PET * N-Phenethylnormorphine * N-Phenethyl-14-ethoxymetopon * Phenomorphan * RAM-378 RAM-378(7,8-Dihydro-14-hydroxy-N-phenethylnormorphine) is an opioid analgesic. It is the N-phenethyl derivative of hydromorphinol Hydromorphinol (RAM-320, 14-hydroxydihydromorphine), is an opiate analogue that is a derivative of morphine, wher ... * Ro4-1539 References 4,5-Epoxymorphinans Semisynthetic opioids Mu-opioid receptor agonists {{Analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Diário Oficial Da União
The ''Diário Oficial da União'' (literally ''Official Diary of the Union''), abbreviated DOU, is the government gazette, official gazette of the Federal Government of Brazil, Federal Government of Brazil. It is published since 1 October 1862 and was created via the Imperial Decree 1,177 of its 9 September as the ''Official Journal of the Empire of Brazil''. Its current name was adopted after Brazil became a federal republic, and the "Union" came into being as the legal personality of the new federal government. The official journal is published by the Imprensa Nacional, Brazilian National Press. Though the journal has been published since 1862, it had many predecessors, as follows: # Gazeta do Rio de Janeiro (10/9/1808 – 29.12.1821) # Gazeta do Rio (1/1/1822 – 31/12/1822) # Diário do Governo (2/1/1823 – 28/6/1833) # Diário Fluminense (21/5/1824 – 24/4/1831) # Correio Oficial (1/7/1833 – 30/6/1836) e (2/1/1830 – 30/12/1840) # Without proper journal (31/12/1840 – ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
N-Phenethylnordesomorphine
''N''-Phenethylnordesomorphine is an opiate analgesic drug derived from desomorphine by replacing the ''N''-methyl group with β-phenethyl. Since desomorphine is already around eight times more potent than morphine, the additional boost in binding affinity produced by using the larger phenethyl group makes ''N''-phenethylnordesomorphine a highly potent analgesic drug, some 85 times more potent than morphine, and a similar strength to the closely related morphinan derivative phenomorphan. See also * 14-Cinnamoyloxycodeinone * 14-Phenylpropoxymetopon * 7-PET * ''N''-Phenethyl-14-ethoxymetopon * ''N''-Phenethylnormorphine * RAM-378 * 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 ... References 4,5-Epoxymorphinans Semisynthetic opioids Mu-opioid receptor agonists ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
