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Other names | Oxymorphone hydrazone |
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Chemical and physical data | |
Formula | C17H21N3O3 |
Molar mass | 315.373 g·mol−1 |
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Oxymorphazone is an opioid analgesic drug related to oxymorphone. Oxymorphazone is a potent and long acting 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]
Clinical data | |
---|---|
Other names | Oxymorphone hydrazone |
ATC code |
|
Identifiers | |
| |
CAS Number | |
PubChem CID | |
ChemSpider | |
UNII | |
Chemical and physical data | |
Formula | C17H21N3O3 |
Molar mass | 315.373 g·mol−1 |
3D model ( JSmol) | |
| |
| |
(verify) |
Oxymorphazone is an opioid analgesic drug related to oxymorphone. Oxymorphazone is a potent and long acting 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]