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Norbinaltorphimine
Introduction
Overview
Overview
Norbinaltorphimine (nor-BNI) is an opioid antagonist used in scientific research. It is one of the few opioid antagonists available that is highly selective for the Îș-opioid receptor, and blocks this receptor without affecting the ÎŒ- or ÎŽ-opioid receptors,[1] although it has less selectivity in vivo than when used in isolated tissues.[2] nor-BNI blocks the effects of kappa agonists in animal models,[3][4] and produces antidepressant effects.[5]
References
References
- â Portoghese PS, Lipkowski AW, Takemori AE. Binaltorphimine and nor-binaltorphimine, potent and selective kappa-opioid receptor antagonists. Life Sciences. 1987 Mar 30;40(13):1287-92. PMID 2882399
- â Birch PJ, Hayes AG, Sheehan MJ, Tyers MB. Norbinaltorphimine: antagonist profile at kappa opioid receptors. European Journal of Pharmacology. 1987 Dec 15;144(3):405-8. PMID 2831070
- â Takemori AE, Ho BY, Naeseth JS, Portoghese PS. Nor-binaltorphimine, a highly selective kappa-opioid antagonist in analgesic and receptor binding assays. Journal of Pharmacology and Experimental Therapeutics. 1988 Jul;246(1):255-8. PMID 2839664
- â Takemori AE, Schwartz MM, Portoghese PS. Suppression by nor-binaltorphimine of kappa opioid-mediated diuresis in rats. Journal of Pharmacology and Experimental Therapeutics. 1988 Dec;247(3):971-4. PMID 2849679
- â Shirayama Y, Ishida H, Iwata M, Hazama GI, Kawahara R, Duman RS. Stress increases dynorphin immunoreactivity in limbic brain regions and dynorphin antagonism produces antidepressant-like effects. Journal of Neurochemistry. 2004 Sep;90(5):1258-68. PMID 15312181