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.
Oxilorphan has some weak partial agonist effects and can produce hallucinogenic effects at high doses, suggesting some kappa opioid agonist action. It was trialled for the treatment of opiate addiction, but was not developed commercially.
^ 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.
^ Sellers EM, Thakur R. Partial agonist properties and toxicity of oral oxilorphan. Journal of Clinical Pharmacology. 1976 Apr;16(4):183-7.
^ 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.
^ 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.
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