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Antidote
Oxilorphan
Другие языки:

    Oxilorphan

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    Oxilorphan
    Oxilorphan.svg
    Clinical data
    ATC code
    • None
    Identifiers
    • (-)-17-(Cyclopropylmethyl)-morphinan-3,14-diol
    CAS Number
    PubChem CID
    ChemSpider
    UNII
    KEGG
    CompTox Dashboard (EPA)
    ECHA InfoCard 100.050.664
    Chemical and physical data
    Formula C20H27NO2
    Molar mass 313.441 g·mol−1
    3D model (JSmol)
    • Oc3ccc4C[C@H]1N(CC[C@@]2(CCCC[C@@]12O)c4c3)CC5CC5
    • InChI=1S/C20H27NO2/c22-16-6-5-15-11-18-20(23)8-2-1-7-19(20,17(15)12-16)9-10-21(18)13-14-3-4-14/h5-6,12,14,18,22-23H,1-4,7-11,13H2/t18-,19+,20-/m1/s1 checkY
    • Key:STBZIDOIKQNFCQ-HSALFYBXSA-N checkY
      (verify)

    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.

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