Norbinaltorphimine
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| Systematic (IUPAC) name | |
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17,17'-(dicyclopropylmethyl)-6,6',7,7'-6,6'-imino- 7,7'-bimorphinan-3,4',14,14'-tetrol
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| Identifiers | |
| CAS Number | 105618-26-6  |
| ATC code | none |
| PubChem | CID 3034416 |
| IUPHAR/BPS | 1642 |
| ChemSpider | 21248347  |
| UNII | 36OOQ86QM1 |
| Chemical data | |
| Formula | C40H43N3O6 |
| Molar mass | 661.784 g/mol |
| 3D model (Jmol) | Interactive image |
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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] although it has less selectivity in vivo than when used in isolated tissues.[2] nor-BNI blocks the effects of κ-opioid agonists in animal models,[3][4] and produces antidepressant effects.[5]
See also[edit]
References[edit]
- ^ 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
- ^ 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
- ^ 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
- ^ 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. doi:10.1111/j.1471-4159.2004.02589.x PMID 15312181
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