Norbuprenorphine
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ECHA InfoCard | 100.208.387 ![]() |
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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]
![](http://upload.wikimedia.org/wikipedia/commons/thumb/e/e0/Buprenorphine_2.png/220px-Buprenorphine_2.png)
Norbuprenorhine
See also[]
References[]
- ^ Yassen A, Kan J, Olofsen E, Suidgeest E, Dahan A, Danhof M (May 2007). "Pharmacokinetic-pharmacodynamic modeling of the respiratory depressant effect of norbuprenorphine in rats". The Journal of Pharmacology and Experimental Therapeutics. 321 (2): 598–607. doi:10.1124/jpet.106.115972. PMID 17283225. S2CID 11921738.
- ^ a b Huang P, Kehner GB, Cowan A, Liu-Chen LY (May 2001). "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. PMID 11303059.
- ^ a b Brown SM, Campbell SD, Crafford A, Regina KJ, Holtzman MJ, Kharasch ED (October 2012). "P-glycoprotein is a major determinant of norbuprenorphine brain exposure and antinociception". J. Pharmacol. Exp. Ther. 343 (1): 53–61. doi:10.1124/jpet.112.193433. PMC 3464040. PMID 22739506.
Categories:
- Drugs not assigned an ATC code
- Morphinans
- Phenols
- Tertiary alcohols
- Ethers
- Kappa-opioid receptor agonists
- Mu-opioid receptor agonists
- Delta-opioid receptor agonists
- Nociceptin receptor agonists
- Opioid metabolites
- Peripherally selective drugs
- Nervous system drug stubs