Norbinaltorphimine (nor-BNI or nBNI) is an opioid 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 it's broad definition in the CSA covering "derivatives". However, no court cases are known to exist for its prosecution and it's possible this could be challenged in court.[9]

See also

References

  1. ^ Munro TA, Huang XP, Inglese C, Perrone MG, Van't Veer A, Carroll FI, et al. (2013-08-14). Porter J (ed.). "Selective κ opioid antagonists nor-BNI, GNTI and JDTic have low affinities for non-opioid receptors and transporters". PLOS ONE. 8 (8): e70701. Bibcode:2013PLoSO...870701M. doi:10.1371/journal.pone.0070701. PMC 3747596. PMID 23976952.
  2. ^ Tyson AS, Khan S, Motiwala Z, Han GW, Zhang Z, Ranjbar M, et al. (January 2025). "Molecular mechanisms of inverse agonism via κ-opioid receptor-G protein complexes". Nature Chemical Biology. doi:10.1038/s41589-024-01812-0. PMID 39775170.
  3. ^ 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): 255–258. doi:10.1016/S0022-3565(25)21011-4. PMID 2839664.
  4. ^ 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): 971–974. doi:10.1016/S0022-3565(25)13309-0. PMID 2849679.
  5. ^ Metcalf MD, Coop A (October 2005). "Kappa opioid antagonists: past successes and future prospects". The AAPS Journal. 7 (3): E704 – E722. doi:10.1208/aapsj070371. PMC 2751273. PMID 16353947.
  6. ^ Potter DN, Damez-Werno D, Carlezon WA, Cohen BM, Chartoff EH (October 2011). "Repeated exposure to the κ-opioid receptor agonist salvinorin A modulates extracellular signal-regulated kinase and reward sensitivity". Biological Psychiatry. 70 (8): 744–753. doi:10.1016/j.biopsych.2011.05.021. PMC 3186866. PMID 21757186.
  7. ^ 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): 1258–1268. doi:10.1111/j.1471-4159.2004.02589.x. PMID 15312181.
  8. ^ 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.
  9. ^ US Drug Enforcement Administration (2024). "Letter to Vice Media Group". Imgur. Archived from the original on 2025-02-07. Retrieved 2025-02-07.
Allikas: https://en.wikipedia.org/wiki/Norbinaltorphimine
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