Oxilorphan Explained

Oxilorphan (INN, USAN) (developmental code name L-BC-2605) is an opioid antagonist of the morphinan family that was never marketed.^[1] 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.^[2] Oxilorphan has some weak partial agonist actions at the MOR (with miosis, nausea, dizziness, and some euphoria observed)^{[3] [4]} and can produce hallucinogenic/dissociative effects at sufficient doses, indicative of KOR activation.^[5] It was trialed for the treatment of opioid addiction, but was not developed commercially.^[6] 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.^[7]

See also

• Butorphanol
• Cyclorphan
• Ketorfanol
• Levallorphan
• Levomethorphan
• Levorphanol
• Nalbuphine
• Proxorphan
• Xorphanol

Notes and References

1. Book: Elks J . The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. 14 November 2014. Springer. 978-1-4757-2085-3. 916–.
2. Pircio AW, Gylys JA . Oxilorphan (l-N-cyclopropylmethyl-3,14-dihydroxymorphinan): a new synthetic narcotic antagonist . The Journal of Pharmacology and Experimental Therapeutics . 193 . 1 . 23–34 . April 1975 . 237112 .
3. Sellers EM, Thakur R . Partial agonist properties and toxicity of oral oxilorphan . Journal of Clinical Pharmacology . 16 . 4 . 183–7 . April 1976 . 4472 . 10.1002/j.1552-4604.1976.tb01515.x . 2819499 .
4. Book: Gordon M . Annual Reports in Medicinal Chemistry . 9 . Abuse of CNS Agents . https://books.google.com/books?id=rZBH1_7Tx6UC&pg=PA41. 22 November 1974. Academic Press. 978-0-08-058353-2. 41–.
5. Leander JD . Evidence that nalorphine, butorphanol and oxilorphan are partial agonists at a kappa-opioid receptor . European Journal of Pharmacology . 86 . 3–4 . 467–70 . January 1983 . 6131829 . 10.1016/0014-2999(83)90198-x .
6. Tennant FS, Tate JA, Ruckel E . Clinical trial in post-addicts with oxilorphan (levo-BC-2605): a new narcotic antagonist . Drug and Alcohol Dependence . 1 . 5 . 329–37 . June 1976 . 13984 . 10.1016/0376-8716(76)90035-1 .
7. Book: National Research Council (U.S.). Committee on Problems of Drug Dependence. Problems of drug dependence. 1975. National Academy of Sciences.. 9780309024174.