Chemistry:5'-Guanidinonaltrindole
From HandWiki
Short description: Chemical compound
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| Other names | 5'-Guanidinonaltrindole, GNTI |
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| Formula | C27H29N5O3 |
| Molar mass | 471.561 g·mol−1 |
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5'-Guanidinonaltrindole (5'-GNTI) is an opioid antagonist used in scientific research which is highly selective for the κ opioid receptor. It is 5x more potent and 500 times more selective than the commonly used κ-opioid antagonist norbinaltorphimine.[1] It has a slow onset and long duration of action,[2][3] and produces antidepressant effects in animal studies.[4] It also increases allodynia by interfering with the action of the κ-opioid peptide dynorphin.[5]
In addition to activity at the KOR, 5'-GNTI has been found to act as a positive allosteric modulator of the α1A-adrenergic receptor (EC50 = 41 nM), and this may contribute to its "severe transient effects".[6]
See also
References
- ↑ "5'-Guanidinonaltrindole, a highly selective and potent kappa-opioid receptor antagonist". European Journal of Pharmacology 396 (1): 49–52. May 2000. doi:10.1016/S0014-2999(00)00208-9. PMID 10822054.
- ↑ "Kappa opioid antagonist effects of the novel kappa antagonist 5'-guanidinonaltrindole (GNTI) in an assay of schedule-controlled behavior in rhesus monkeys". Psychopharmacology 163 (3–4): 412–9. October 2002. doi:10.1007/s00213-002-1038-x. PMID 12373442.
- ↑ "Long-acting kappa opioid antagonists disrupt receptor signaling and produce noncompetitive effects by activating c-Jun N-terminal kinase". The Journal of Biological Chemistry 282 (41): 29803–11. October 2007. doi:10.1074/jbc.M705540200. PMID 17702750.
- ↑ "Antidepressant-like effects of kappa-opioid receptor antagonists in the forced swim test in rats". The Journal of Pharmacology and Experimental Therapeutics 305 (1): 323–30. April 2003. doi:10.1124/jpet.102.046433. PMID 12649385.
- ↑ "Antagonists of the kappa-opioid receptor enhance allodynia in rats and mice after sciatic nerve ligation". British Journal of Pharmacology 140 (3): 538–46. October 2003. doi:10.1038/sj.bjp.0705427. PMID 12970097.
- ↑ "Selective κ opioid antagonists nor-BNI, GNTI and JDTic have low affinities for non-opioid receptors and transporters". PLOS ONE 8 (8): e70701. 2013. doi:10.1371/journal.pone.0070701. PMID 23976952. Bibcode: 2013PLoSO...870701M.
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