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Levomoramide
Levomoramide is the inactive isomer of the opioid analgesic dextromoramide, invented by the chemist Paul Janssen in 1956. Unlike dextromoramide, which is a potent analgesic with high abuse potential, levomoramide is virtually without activity. "Resolution reveals that the analgetic activity in this case resides almost entirely in the (+) isomer." "In the α-CH3 series, one of the optical isomers of each enantiomorphic pair is about twice as active as the racemic mixture; the other isomer is devoid of significant analgesic activity." However, despite being inactive, levomoramide is scheduled by UN Single Convention on Narcotic Drugs The Single Convention on Narcotic Drugs, 1961 (Single Convention, 1961 Convention, or C61) is an international treaty that controls activities (cultivation, production, supply, trade, transport) of specific narcotic drugs and lays down a syst .... References Synthetic opioids 4-Morpholinyl compunds Pyrrolidines Carboxamides {{organic- ...
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Synthetic 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 ...
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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 back-for ...
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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 th ...
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Paul Janssen
Paul Adriaan Jan, Baron Janssen (12 September 1926 - 11 November 2003) was a Belgian physician. He was the founder of Janssen Pharmaceutica, a pharmaceutical company with over 20,000 employees which is now a subsidiary of Johnson & Johnson. Early life and education Paul Janssen was the son of Constant Janssen and Margriet Fleerackers. He attended secondary school at the Jesuit St Jozef college in Turnhout, Belgium after which he decided to follow in his father's footsteps and become a physician. During World War II Janssen studied physics, biology and chemistry at the Facultés universitaires Notre-Dame de la Paix (FUNDP) in Namur. He then studied medicine at the Catholic University of Leuven and Ghent University. In 1951, Janssen received his medical degree ''magna cum laude'' from Ghent University. He graduated with a postdoctoral degree in pharmacology at the same university in 1956, and studied at the Institute of Pharmacology of the University of Cologne. On 16 April 195 ...
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United Nations
The United Nations (UN) is an intergovernmental organization whose stated purposes are to maintain international peace and international security, security, develop friendly relations among nations, achieve international cooperation, and be a centre for harmonizing the actions of nations. It is the world's largest and most familiar international organization. The UN is headquarters of the United Nations, headquartered on extraterritoriality, international territory in New York City, and has other main offices in United Nations Office at Geneva, Geneva, United Nations Office at Nairobi, Nairobi, United Nations Office at Vienna, Vienna, and Peace Palace, The Hague (home to the International Court of Justice). The UN was established after World War II with Dumbarton Oaks Conference, the aim of preventing future world wars, succeeding the League of Nations, which was characterized as ineffective. On 25 April 1945, 50 governments met in San Francisco for United Nations Conference ...
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Single Convention On Narcotic Drugs
The Single Convention on Narcotic Drugs, 1961 (Single Convention, 1961 Convention, or C61) is an international treaty that controls activities (cultivation, production, supply, trade, transport) of specific narcotic drugs and lays down a system of regulations (licenses, measures for treatment, research, etc.) for their medical and scientific uses; it also establishes the International Narcotics Control Board. The Single Convention was adopted in 1961 and amended in 1972. As of 2022, the Single Convention as amended has been ratified by 186 countries. The convention has since been supplemented by the 1971 Convention on Psychotropic Substances, which controls LSD, MDMA, and other psychoactive pharmaceuticals, and the 1988 United Nations Convention Against Illicit Traffic in Narcotic Drugs and Psychotropic Substances. Ratification The Single Convention as amended in 1972 had been ratified or acceded to by 186 states. Only Chad remained party to the original 1961 Convention ...
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Pyrrolidines
Pyrrolidine, also known as tetrahydropyrrole, is an organic compound with the molecular formula (CH2)4NH. It is a cyclic secondary amine, also classified as a saturated heterocycle. It is a colourless liquid that is miscible with water and most organic solvents. It has a characteristic odor that has been described as "ammoniacal, fishy, shellfish-like". In addition to pyrrolidine itself, many substituted pyrrolidines are known. Production and synthesis Industrial production Pyrrolidine is prepared industrially by the reaction of 1,4-butanediol and ammonia at a temperature of 165–200 °C and a pressure of 17–21 MPa in the presence of a cobalt- and nickel oxide catalyst, which is supported on alumina. : The reaction is carried out in the liquid phase in a continuous tube- or tube bundle reactor, which is operated in the cycle gas method. The catalyst is arranged as a fixed-bed and the conversion is carried out in the downflow mode. The product is obtained after mu ...
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