|
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 * 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. ... [...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] |
Semisynthetic 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] |
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 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 * 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 ... References 4,5-Epoxymorphinans Semisynthetic opioids Mu-opioid receptor agonists {{Analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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, 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] |
MR-2096
MR-2096 is a relatively weak opioid analgesic. It has an unusual chiral tetrahydrofuran-2-ylmethyl substitution on the nitrogen which determines the character of effects and toxicity, with the (R) enantiomer MR-2096 being an opioid agonist, while the (S) enantiomer MR-2097 has similarly potent opioid antagonist effects. This substitution makes MR 2096 completely synthetic. It does not require the use of any opium derivatives to produce. This mix of activities has made these two enantiomers useful for characterising the binding site of the mu opioid receptor. It was never marketed due to its high toxicity. See also * N-Phenethylnormorphine * 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 ... References 4,5-Epoxymorphinans Phenols Ketones Ethers Mu-opioid re ... [...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 0.16nM at μ and 3.14nM at δ. See also * 14-Cinnamoyloxycodeinone * 14-Phenylpropoxymetopon * 7-PET * MR-2096 * N-Phenethylnormorphine * Phenomorphan * 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 t ... References Delta-opioid receptor agonists 4,5-Epoxymorphinans Phenols Ketones Ethers Mu-opioid receptor agonists Semisynthetic opioids {{analgesic-stub ... [...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 85x 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 t ... References 4,5-Epoxymorphinans Semisynthetic opioids Mu-opioid receptor agonists ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 * 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 t ... [...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. See also * 14-Cinnamoyloxycodeinone * 14-Phenylpropoxymetopon * 7-PET * N-Phenethylnormorphine * N-Phenethyl-14-ethoxymetopon * Phenomorphan * 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 ... References 4,5-Epoxymorphinans Semisynthetic opioids {{Analgesic-stub ... [...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. See also * 14-Cinnamoyloxycodeinone * 14-Phenylpropoxymetopon * 7 ... [...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'' ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 other illicit drug, illicit opioids. There are numerous methods used to administer morphine: oral; sublingual administration, sublingual; via inhalation; intramuscular, injection into a muscle; by Subcutaneous injection, injection under the skin; intravenously; Intrathecally, injection into the space around the spinal cord; transdermal; or via rectal administration, rectal suppository. It acts directly on the central nervous system (CNS) to induce analgesia and alter perception and emotional response to pain. Physical and psychological dependence and tolerance may develop with repeated administration. It can be taken for both acute pain and chronic pain and is frequently used for pain from myocardial infarction, kidney stones, and during Ch ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
