Chemistry:Norbuprenorphine
From HandWiki
Short description: Active metabolite of buprenorphine
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| Formula | C25H35NO4 |
| Molar mass | 413.558 g·mol−1 |
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Norbuprenorphine is a major active metabolite of the opioid modulator buprenorphine. It is a μ-opioid, δ-opioid, and nociceptin receptor full agonist,[1][2] and a κ-opioid receptor partial agonist.[2] In rats, unlike buprenorphine, norbuprenorphine produces marked respiratory depression but with very little antinociceptive effect.[3] In explanation of these properties, norbuprenorphine has been found to be a high affinity P-glycoprotein substrate, and in accordance, shows very limited blood-brain-barrier penetration.[3]
See also
References
- ↑ "Pharmacokinetic-pharmacodynamic modeling of the respiratory depressant effect of norbuprenorphine in rats". The Journal of Pharmacology and Experimental Therapeutics 321 (2): 598–607. May 2007. doi:10.1124/jpet.106.115972. PMID 17283225.
- ↑ 2.0 2.1 "Comparison of pharmacological activities of buprenorphine and norbuprenorphine: norbuprenorphine is a potent opioid agonist". The Journal of Pharmacology and Experimental Therapeutics 297 (2): 688–95. May 2001. PMID 11303059. http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=11303059.
- ↑ 3.0 3.1 "P-glycoprotein is a major determinant of norbuprenorphine brain exposure and antinociception". J. Pharmacol. Exp. Ther. 343 (1): 53–61. October 2012. doi:10.1124/jpet.112.193433. PMID 22739506.
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