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Buprenorphine


Mechanism of action:

Buprenorphine is an opioid that acts as a partial agonist at the μ-opioid receptor and an antagonist at the κ-opioid receptor. Buprenorphine binds to μ-opioid receptors with high affinity and produces receptor signaling associated with analgesia. However, at higher doses, it exhibits a ceiling effect, causing μ-receptor-related effects to plateau. Because of this property, it can also be used in treatment strategies related to opioid dependence. In addition, inhibition of the κ-opioid receptor can modulate κ-receptor-associated neural signaling.

Reference(s):

1. Huang P et al. (2001). Comparison of pharmacological activities of buprenorphine and norbuprenorphine: norbuprenorphine is a potent opioid agonist. J Pharmacol Exp Ther. 


2. Bodkin JA et al. (1995). Buprenorphine treatment of refractory depression. J Clin Psychopharmacol. 


3. Elkader A et al. (2005). Buprenorphine: clinical pharmacokinetics in the treatment of opioid dependence. Clin Pharmacokinet.

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