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8-Carboxamidocyclazocine : ウィキペディア英語版 | 8-Carboxamidocyclazocine
8-Carboxamidocyclazocine (8-CAC) is an opioid analgesic drug related to cyclazocine, invented by medicinal chemist Mark P. Wentland and co-workers in Cogswell Laboratory at Rensselaer Polytechnic Institute.〔US Patent 6784187 8-carboxamido-2,6-methano-3-benzazocines〕 Similarly to cyclazocine, 8-CAC acts as an agonist at both the μ and κ opioid receptors, but has a much longer duration of action than cyclazocine, and does not have μ antagonist activity. Unexpectedly it was discovered that the phenolic hydroxyl group of cyclazocine could be replaced by a carboxamido group with only slight loss of potency at opioid receptors, and this discovery has subsequently been used to develop a large number of novel opioid derivatives where the phenolic hydroxy group has been replaced by either carboxamide or a variety of larger groups. Due to their strong κ-opioid agonist activity, these drugs are not suited for use as analgesics in humans, but have instead been researched as potential drugs for the treatment of cocaine addiction. ==See also==
* Samidorphan
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