Chemistry:GR-89696
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Short description: Chemical compound
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| Formula | C19H25Cl2N3O3 |
| Molar mass | 414.33 g·mol−1 |
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GR-89696 is a drug which acts as a highly selective κ-opioid agonist.[1] It has been studied in various animal species, and has been described as selective for the κ2 subtype.[2][3][4] Recent studies have suggested that GR-89696 and related κ2-selective agonists may be useful for preventing the itching which is a common side effect of conventional opioid analgesic drugs, without the additional side effects of non-selective kappa agonists.[5] The structure bound to the κ-opioid receptor has been reported.[6]
References
- ↑ "A potent new class of kappa-receptor agonist: 4-substituted 1-(arylacetyl)-2-[(dialkylamino)methyl]piperazines". Journal of Medicinal Chemistry 36 (15): 2075–2083. July 1993. doi:10.1021/jm00067a004. PMID 8393489.
- ↑ "Functional evidence for multiple receptor activation by kappa-ligands in the inhibition of spinal nociceptive reflexes in the rat". British Journal of Pharmacology 110 (1): 303–309. September 1993. doi:10.1111/j.1476-5381.1993.tb13809.x. PMID 8220893.
- ↑ "Putative kappa-2 opioid agonists are antihyperalgesic in a rat model of inflammation". The Journal of Pharmacology and Experimental Therapeutics 281 (1): 136–141. April 1997. PMID 9103490.
- ↑ "GR89,696: a potent kappa-opioid agonist with subtype selectivity in rhesus monkeys". The Journal of Pharmacology and Experimental Therapeutics 298 (3): 1049–1059. September 2001. PMID 11504802.
- ↑ "Effects of atypical kappa-opioid receptor agonists on intrathecal morphine-induced itch and analgesia in primates". The Journal of Pharmacology and Experimental Therapeutics 328 (1): 193–200. January 2009. doi:10.1124/jpet.108.143925. PMID 18842704.
- ↑ "Ligand and G-protein selectivity in the κ-opioid receptor". Nature 617 (7960): 417–425. May 2023. doi:10.1038/s41586-023-06030-7. PMID 37138078. Bibcode: 2023Natur.617..417H.
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