Chemistry:Norbinaltorphimine
Norbinaltorphimine (nor-BNI or nBNI) is an opioid receptor antagonist used in scientific research. It is a highly selective inverse agonist for the κ-opioid receptor.[1][2] In animals, nor-BNI blocks the effects of κ-opioids[3][4] with a slow onset and an exceptionally long duration of action (up to several months).[5][6] It produces antidepressant-like[7] and anxiolytic-like effects in animal models.[8]
Legality
In the United States, a letter from Terrence L. Boos, Ph.D., Chief Drug & Chemical Evaluation Section Diversion Control Division at the DEA shows they consider nor-BNI a Schedule II substance as a derivative of noroxymorphone due to its broad definition in the CSA covering "derivatives". However, no court cases are known to exist for its prosecution and it is possible this could be challenged in court.[9]
See also
References
- ↑ "Selective κ opioid antagonists nor-BNI, GNTI and JDTic have low affinities for non-opioid receptors and transporters". PLOS ONE 8 (8). 2013-08-14. doi:10.1371/journal.pone.0070701. PMID 23976952. Bibcode: 2013PLoSO...870701M.
- ↑ "Molecular mechanisms of inverse agonism via κ-opioid receptor-G protein complexes". Nature Chemical Biology 21 (7): 1046–1057. January 2025. doi:10.1038/s41589-024-01812-0. PMID 39775170.
- ↑ "Nor-binaltorphimine, a highly selective kappa-opioid antagonist in analgesic and receptor binding assays". The Journal of Pharmacology and Experimental Therapeutics 246 (1): 255–258. July 1988. doi:10.1016/S0022-3565(25)21011-4. PMID 2839664.
- ↑ "Suppression by nor-binaltorphimine of kappa opioid-mediated diuresis in rats". The Journal of Pharmacology and Experimental Therapeutics 247 (3): 971–974. December 1988. doi:10.1016/S0022-3565(25)13309-0. PMID 2849679.
- ↑ "Kappa opioid antagonists: past successes and future prospects". The AAPS Journal 7 (3): E704–E722. October 2005. doi:10.1208/aapsj070371. PMID 16353947.
- ↑ "Repeated exposure to the κ-opioid receptor agonist salvinorin A modulates extracellular signal-regulated kinase and reward sensitivity". Biological Psychiatry 70 (8): 744–753. October 2011. doi:10.1016/j.biopsych.2011.05.021. PMID 21757186.
- ↑ "Stress increases dynorphin immunoreactivity in limbic brain regions and dynorphin antagonism produces antidepressant-like effects". Journal of Neurochemistry 90 (5): 1258–1268. September 2004. doi:10.1111/j.1471-4159.2004.02589.x. PMID 15312181.
- ↑ "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. June 2017. doi:10.1016/j.bbr.2017.03.033. PMID 28347824.
- ↑ US Drug Enforcement Administration (2024). "Letter to Vice Media Group" (in en). https://imgur.com/a/giJPW6u.
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