Norbuprenorphine
Norbuprenorphine is an active metabolite of the opioid modulator buprenorphine. It is a partial agonist at the mu-opioid receptor and an antagonist at the kappa-opioid receptor. Norbuprenorphine has been found to possess analgesic effects and may contribute to the overall analgesic effects of buprenorphine.
Pharmacology[edit | edit source]
Norbuprenorphine is a major metabolite of buprenorphine, produced by N-dealkylation via CYP3A4 enzymes in the liver. It has been found to bind strongly to mu-opioid receptors and kappa-opioid receptors, acting as a partial agonist and antagonist, respectively. This activity at opioid receptors leads to its analgesic effects.
Clinical significance[edit | edit source]
The clinical significance of norbuprenorphine is not fully understood. It is known to be a potent analgesic, and it is thought to contribute to the overall analgesic effect of buprenorphine. However, its role in the side effects of buprenorphine treatment is not clear.
See also[edit | edit source]
References[edit | edit source]
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