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Desmethylmoramide
Desmethylmoramide (INN) is an opioid analgesic related to dextromoramide (the active (+)-isomer of moramide) that was synthesized and characterized in the late 1950s but was never marketed. Synthesis The starting diphenylacetylpyrrolidine 0678-46-8can be made in ~84% yield by the reaction of methyldiphenylacetate with pyrrolidine. Or ~62% from amidation of the free acid (by Schotten-Baumann reaction). See also * Dipyanone * Nufenoxole * Phenadoxone Phenadoxone (trade names Heptalgin, Morphidone, and Heptazone) is an opioid analgesic of the open chain class (methadone and relatives) invented in Germany by Hoechst in 1947. It is one of a handful of useful synthetic analgesics which were used ... References Further reading * 4-Morpholinyl compunds Opioids {{analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Desmethylmoramide Synthesis
Desmethylmoramide (International Nonproprietary Name, INN) is an opioid analgesic related to dextromoramide (the active (+)-isomer of moramide) that was synthesized and characterized in the late 1950s but was never marketed. Synthesis The starting diphenylacetylpyrrolidine [60678-46-8] can be made in ~84% yield by the reaction of methyldiphenylacetate with pyrrolidine. Or ~62% from amidation of the free acid (by Schotten-Baumann reaction). See also * Dipyanone * Nufenoxole * Phenadoxone References Further reading * 4-Morpholinyl compunds Opioids {{analgesic-stub ... [...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* IC-26 IC-26 (WIN 1161-3, Methiodone) is an analogue of the opioid analgesic methadone, where the carbonyl group has been replaced by the bioisosteric sulfone group. Human and animal studies suggest that IC-26 is around the same potency as methadone ... * Nufenoxole * Pyrrolidinylthiambutene References Opioids Pyrrolidines Mu-opioid receptor agonists Ketones {{analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nufenoxole
Nufenoxole (SC-27166) is an antidiarrhoeal drug which acts as a peripherally selective opioid agonist, in a similar manner to loperamide and diphenoxylate. While it is able to activate μ-opioid receptors, it fails to cross the blood–brain barrier and so has a selective action against diarrhoea without producing analgesic effects. See also * Dipipanone * 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 References Antidiarrhoeals Mu-opioid receptor agonists Oxadiazoles Peripherally selective drugs {{pharm-stub ... [...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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Analgesic
An analgesic drug, also called simply an analgesic (American English), analgaesic (British English), pain reliever, or painkiller, is any member of the group of drugs used to achieve relief from pain (that is, analgesia or pain management). It is typically used to induce cooperation with a medical procedure. Analgesics are conceptually distinct from anesthetics, which temporarily reduce, and in some instances eliminate, sensation, although analgesia and anesthesia are neurophysiologically overlapping and thus various drugs have both analgesic and anesthetic effects. Analgesic choice is also determined by the type of pain: For neuropathic pain, traditional analgesics are less effective, and there is often benefit from classes of drugs that are not normally considered analgesics, such as tricyclic antidepressants and anticonvulsants. Various analgesics, such as many NSAIDs, are available over the counter in most countries, whereas various others are prescription drugs owi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dextromoramide
Dextromoramide (Palfium, Palphium, Jetrium, Dimorlin) is a powerful opioid analgesic approximately three times more potent than morphine but shorter acting. It is subject to drug prohibition regimes, both internationally through UN treaties and by the criminal law of individual states, and is usually prescribed only in the Netherlands. History Dextromoramide was discovered and patented in 1956 by Dr Paul Janssen at Janssen Pharmaceutica, who also discovered fentanyl, another important synthetic opioid, widely used to treat pain and in combination with other drugs as an anaesthetic, as well as haloperidol, piritramide, the loperamide- diphenoxylate series and other important drugs. Dextromoramide was much favoured by drug users in Australia in the 1970s and the United Kingdom. It has the main proprietary name of Palfium amongst others, though as of mid-2004 the drug was discontinued in the UK due to limited supplies of precursor chemicals. Although this is true, it is believed ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Isomer
In chemistry, isomers are molecules or polyatomic ions with identical molecular formulae – that is, same number of atoms of each element – but distinct arrangements of atoms in space. Isomerism is existence or possibility of isomers. Isomers do not necessarily share similar chemical or physical properties. Two main forms of isomerism are structural or constitutional isomerism, in which '' bonds'' between the atoms differ; and stereoisomerism or spatial isomerism, in which the bonds are the same but the ''relative positions'' of the atoms differ. Isomeric relationships form a hierarchy. Two chemicals might be the same constitutional isomer, but upon deeper analysis be stereoisomers of each other. Two molecules that are the same stereoisomer as each other might be in different conformational forms or be different isotopologues. The depth of analysis depends on the field of study or the chemical and physical properties of interest. The English word "isomer" () is a bac ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Moramide
Racemoramide (INN, BAN), or simply moramide, is an opioid analgesic and a racemic mixture of the substances dextromoramide (the active component) and levomoramide (which is inactive), two enantiomers of a chiral molecule. Racemoramide is itself controlled; in the United States it is under Schedule I as a Narcotic with an ACSCN of 9645 and a zero annual aggregate manufacturing quota as of 2014. Its salts are the bitartrate (free base conversion ratio 0.723) and dihydrochloride (0.843) Moramide intermediate Moramide intermediate (3-methyl-4-morpholin-4-yl-2,2-diphenylbutanoic acid, on INCB Yellow List as 2-methyl-3-morpholino-1,1-diphenylpropane carboxylic acid) is a moramide precursor scheduled by UN Single Convention on Narcotic Drugs. In the Un ... is listed separately as a Schedule II Narcotic controlled substance (ACSCN 9802), also with a zero quota. References Analgesics 4-Morpholinyl compunds Opioids Propionamides Pyrrolidines {{analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Phenadoxone
Phenadoxone (trade names Heptalgin, Morphidone, and Heptazone) is an opioid analgesic of the open chain class (methadone and relatives) invented in Germany by Hoechst in 1947. It is one of a handful of useful synthetic analgesics which were used in the United States for various lengths of time in the 20 or so years after the end of the Second World War but which were withdrawn from the market for various or no known reason and which now are mostly in Schedule I of the United States' Controlled Substances Act of 1970, or (like phenazocine and bezitramide) in Schedule II but not produced or marketed in the US. Others on this list are ketobemidone (Ketogin), dextromoramide (Dimorlin, Palfium and others), phenazocine (Narphen and Prinadol), dipipanone (Diconal, Pipadone and Wellconal), piminodine (Alvodine), propiram (Algeril), anileridine (Leritine) and alphaprodine (Nisentil). Phenadoxone has a US DEA ACSCN of 9637 and recently has had a zero annual manufacturing quota under the C ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
