Oxilorphan (INN, USAN) (developmental code name L-BC-2605) is an opioid antagonist of the morphinan family that was never marketed. It acts as a μ-opioid receptor (MOR) antagonist but a κ-opioid receptor (KOR) partial agonist, and has similar effects to naloxone and around the same potency as an MOR antagonist. Oxilorphan has some weak partial agonist actions at the MOR (with miosis, nausea, dizziness, and some euphoria observed) and can produce hallucinogenic/dissociative effects at sufficient doses, indicative of KOR activation. It was trialed for the treatment of opioid addiction, but was not developed commercially. The KOR agonist effects of oxilorphan are associated with dysphoria, which combined with its hallucinogenic effects, serve to limit its clinical usefulness; indeed, many patients who experienced these side effects refused to take additional doses in clinical trials.
|Chemical and physical data|
|Molar mass||313.44 g/mol g·mol−1|
|3D model (JSmol)|
- J. Elks (14 November 2014). The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. pp. 916–. ISBN 978-1-4757-2085-3.
- 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.
- ANNUAL REPORTS IN MED CHEMISTRY V9 PPR. Academic Press. 22 November 1974. pp. 41–. ISBN 978-0-08-058353-2.
- 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.
- National Research Council (U.S.). Committee on Problems of Drug Dependence (1975). Problems of drug dependence. National Academy of Sciences.
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