Nalorphine ( INN Tooltip International Nonproprietary Name ) (brand names Lethidrone , Nalline ), also known as N -allylnormorphine , is a mixed opioid agonist–antagonist with opioid antagonist and analgesic properties. It was introduced in 1954 and was used as an antidote to reverse opioid overdose and in a challenge test to determine opioid dependence .
4-427: Nalorphine was the second opioid antagonist to be introduced, preceded by nalodeine ( N -allylnorcodeine) in 1915 and followed by naloxone in 1960 and naltrexone in 1963. Due to potent activation of the κ-opioid receptor , nalorphine produces side effects such as dysphoria , anxiety , confusion , and hallucinations , and for this reason, is no longer used medically. Nalorphine acts at two opioid receptors —
8-574: A number of others as well as a number of codeine -based analogues. More recently, it has become much more commonplace to use ethyl chloroformate instead of cyanogen bromide for the Von Braun degradation demethylation step. See for example the list of phenyltropanes or the synthesis of paroxetine for further examples of this. This analgesic -related article is a stub . You can help Misplaced Pages by expanding it . Nalodeine Nalodeine , also known more commonly as N-allylnorcodeine ,
12-571: Is an opioid antagonist (specifically, an antagonist of the μ-opioid receptor ) that was never marketed but is notable as the first opioid antagonist to be discovered. It was first reported in 1915 and was found to block the effects of morphine in animals. This was followed by the clinical introduction of nalorphine (N-allylnor morphine ) in 1954, naloxone (N-allyl oxymorphone ) in 1960, and naltrexone (N-methylcyclopropyloxymorphone) in 1963. Nalmefene (6-desoxy-6-methylene-naltrexone), another structurally related opioid antagonist derivative,
16-431: The μ-opioid receptor (MOR) where it has antagonistic effects, and at the κ-opioid receptor (KOR) (K i = 1.6 nM; EC 50 = 483 nM; E max = 95%) where it exerts high- efficacy partial agonist /near- full agonist characteristics. Nalorphine has a number of analogues including niconalorphine (the nicomorphine analogue), diacetylnalorphine ( heroin analogue), dihydronalorphine (dihydromorphine), and
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