Norbinaltorphimine
Norbinaltorphimine (nor-BNI or nBNI) is an opioid antagonist used in scientific research. It is one of the few opioid antagonists available that is highly selective for the κ-opioid receptor, and blocks this receptor without affecting the μ- or δ-opioid receptors,[1][2] although it has less selectivity in vivo than when used in isolated tissues.[3] nor-BNI blocks the effects of κ-opioid agonists in animal models,[4][5] and produces antidepressant[6] and antipanic-like effects.[2]
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Formula | C40H43N3O6 |
Molar mass | 661.799 g·mol−1 |
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References
- Portoghese PS, Lipkowski AW, Takemori AE (March 1987). "Binaltorphimine and nor-binaltorphimine, potent and selective kappa-opioid receptor antagonists". Life Sciences. 40 (13): 1287–92. doi:10.1016/0024-3205(87)90585-6. PMID 2882399.
- Maraschin JC, Almeida CB, Rangel MP, Roncon CM, Sestile CC, Zangrossi H, et al. (June 2017). "Participation of dorsal periaqueductal gray 5-HT1A receptors in the panicolytic-like effect of the κ-opioid receptor antagonist Nor-BNI". Behavioural Brain Research. 327: 75–82. doi:10.1016/j.bbr.2017.03.033. PMID 28347824. S2CID 22465963.
- Birch PJ, Hayes AG, Sheehan MJ, Tyers MB (December 1987). "Norbinaltorphimine: antagonist profile at kappa opioid receptors". European Journal of Pharmacology. 144 (3): 405–8. doi:10.1016/0014-2999(87)90397-9. PMID 2831070.
- Takemori AE, Ho BY, Naeseth JS, Portoghese PS (July 1988). "Nor-binaltorphimine, a highly selective kappa-opioid antagonist in analgesic and receptor binding assays". The Journal of Pharmacology and Experimental Therapeutics. 246 (1): 255–8. PMID 2839664.
- Takemori AE, Schwartz MM, Portoghese PS (December 1988). "Suppression by nor-binaltorphimine of kappa opioid-mediated diuresis in rats". The Journal of Pharmacology and Experimental Therapeutics. 247 (3): 971–4. PMID 2849679.
- Shirayama Y, Ishida H, Iwata M, Hazama GI, Kawahara R, Duman RS (September 2004). "Stress increases dynorphin immunoreactivity in limbic brain regions and dynorphin antagonism produces antidepressant-like effects". Journal of Neurochemistry. 90 (5): 1258–68. doi:10.1111/j.1471-4159.2004.02589.x. PMID 15312181.
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