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Oxilorphan is an opioid antagonist from the morphinan family of drugs. Oxilorphan is a non-selective opioid which is a μ antagonist but a κ partial agonist. It has similar effects to naloxone, and around the same potency as an antagonist.〔Pircio AW, Gylys JA. Oxilorphan (l-N-cyclopropylmethyl-3,14-dihydroxymorphinan): a new synthetic narcotic antagonist. ''Journal of Pharmacology and Experimental Therapeutics''. 1975 Apr;193(1):23-34.〕 Oxilorphan has some weak partial agonist effects〔Sellers EM, Thakur R. Partial agonist properties and toxicity of oral oxilorphan. ''Journal of Clinical Pharmacology''. 1976 Apr;16(4):183-7.〕 and can produce hallucinogenic/dissociative effects at high doses, suggesting some kappa opioid agonist action.〔Leander JD. Evidence that nalorphine, butorphanol and oxilorphan are partial agonists at a kappa-opioid receptor. ''European Journal of Pharmacology''. 1983 Jan 21;86(3-4):467-70.〕 It was trialled for the treatment of opiate addiction, but was not developed commercially.〔Tennant FS Jr, Tate JA, Ruckel E. Clinical trial in post-addicts with oxilorphan (levo-BC-2605): a new narcotic antagonist. ''Drug and Alcohol Dependence''. 1976 Jun;1(5):329-37.〕 Oxilorphan's mu-opioid antagonist and kappa-opioid agonist effects are associated with dysphoria, which combined with the hallucinogenic properties of kappa-opioid agonism limit the clinical usefulness of the drug. == See also == * Morphinan * Dextrallorphan 抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)』 ■ウィキペディアで「Oxilorphan」の詳細全文を読む スポンサード リンク
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