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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] |
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 potent and its oral bioavailability is fairly low. Generally, Metopon has few advantages to distinguish it from other, more commonly used opioid analgesics, although it does have a slightly lower tendency to produce nausea and respiratory depression compared to morphine. In Canada, as of 1948, the hydrochloride of metopon (free base conversion ratio 0.891, molecular weight 335.8) was available only for oral administration for malignant pain and for maintenance of those habituated to morphine; the only dosage form available was singly scored 8 mg tablets. It was manufactured by Parke, Davis, & Co., and was only for sale to doctors and hospitals. Parke, Davis & Co. did not sell metopon to pharmacies. It is unknown whether metopon tab ... [...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 ... [...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 * ... [...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 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 ... * N-Phenethylnormorphine * N-Phenethyl-14-ethoxymetopon * Phenomorphan * RAM-378 * Ro4-1539 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 tachy ... [...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 An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the ag ..., 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 contr ... [...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] |
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] |
Ethers
In organic chemistry, ethers are a class of compounds that contain an ether group—an oxygen atom connected to two alkyl or aryl groups. They have the general formula , where R and R′ represent the alkyl or aryl groups. Ethers can again be classified into two varieties: if the alkyl or aryl groups are the same on both sides of the oxygen atom, then it is a simple or symmetrical ether, whereas if they are different, the ethers are called mixed or unsymmetrical ethers. A typical example of the first group is the solvent and anaesthetic diethyl ether, commonly referred to simply as "ether" (). Ethers are common in organic chemistry and even more prevalent in biochemistry, as they are common linkages in carbohydrates and lignin. Structure and bonding Ethers feature bent C–O–C linkages. In dimethyl ether, the bond angle is 111° and C–O distances are 141 pm. The barrier to rotation about the C–O bonds is low. The bonding of oxygen in ethers, alcohols, and water is ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ketones
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 bond C=O). The simplest ketone is acetone (where R and R' is methyl), with the formula . Many ketones are of great importance in biology and in industry. Examples include many sugars ( ketoses), many steroids (e.g., testosterone), and the solvent acetone. Nomenclature and etymology The word ''ketone'' is derived from ''Aketon'', an old German word for ''acetone''. According to the rules of IUPAC nomenclature, ketone names are derived by changing the suffix ''-ane'' of the parent alkane to ''-anone''. Typically, the position of the carbonyl group is denoted by a number, but traditional nonsystematic names are still generally used for the most important ketones, for example acetone and benzophenone. These nonsystematic names are considered ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Phenols
In organic chemistry, phenols, sometimes called phenolics, are a class of chemical compounds consisting of one or more hydroxyl groups (— O H) bonded directly to an aromatic hydrocarbon group. The simplest is phenol, . Phenolic compounds are classified as simple phenols or polyphenols based on the number of phenol units in the molecule. Phenols are both synthesized industrially and produced by plants and microorganisms. Properties Acidity Phenols are more acidic than typical alcohols. The acidity of the hydroxyl group in phenols is commonly intermediate between that of aliphatic alcohols and carboxylic acids (their pKa is usually between 10 and 12). Deprotonation of a phenol forms a corresponding negative phenolate ion or phenoxide ion, and the corresponding salts are called phenolates or phenoxides (aryloxides according to the IUPAC Gold Book). Condensation with aldehydes and ketones Phenols are susceptible to Electrophilic aromatic substitutions. Condensation with form ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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