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

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

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

• Buprenorphine
• Opioid receptor
• CYP3A4

References

Norbuprenorphine Resources
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