Oxilorphan

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Oxilorphan
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Clinical data
SynonymsOxilorphan
Identifiers
CAS Number
PubChem CID
E number{{#property:P628}}
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Chemical and physical data
FormulaC20H27NO2
Molar mass313.44 g/mol

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.[1]

Oxilorphan has some weak partial agonist effects[2] and can produce hallucinogenic effects at high doses, suggesting some kappa opioid agonist action.[3] It was trialled for the treatment of opiate addiction, but was not developed commercially.[4]



References

  1. 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.
  2. Sellers EM, Thakur R. Partial agonist properties and toxicity of oral oxilorphan. Journal of Clinical Pharmacology. 1976 Apr;16(4):183-7.
  3. 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.
  4. 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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