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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,〔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〕 although it has less selectivity ''in vivo'' than when used in isolated tissues.〔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〕 nor-BNI blocks the effects of κ-opioid agonists in animal models,〔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〕〔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〕 and produces antidepressant effects.〔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〕
==See also==
* Binaltorphimine
* 5'-Guanidinonaltrindole
* JDTic
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