Oxymorphazone
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Other names | Oxymorphone hydrazone |
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Oxymorphazone is an
μ-opioid agonist which binds irreversibly to the receptor, forming a covalent bond which prevents it from detaching once bound.[1][2] This gives it an unusual pharmacological profile, and while oxymorphazone is only around half the potency of oxymorphone, with higher doses the analgesic effect becomes extremely long lasting, with a duration of up to 48 hours.[3] However, tolerance to analgesia develops rapidly with repeated doses,[4][5][6] as chronically activated opioid receptors are rapidly internalised by β-arrestins, similar to the results of non-covalent binding by repeated doses of agonists with extremely high binding affinity such as lofentanil.[7][8]
See also
- Chlornaltrexamine, an irreversible mixed μ-opioid agonist-antagonist
- Chloroxymorphamine, another irreversible μ-opioid full agonist
- Naloxazone, an irreversible μ-opioid antagonist