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GYKI-46903 is a non-competitive antagonist for 5-HT3 receptors. In displacement studies, the pIC50 values of GYKI-46903 against [3H]granisetron binding to rat cerebral cortex membranes were 6.91. GYKI-46903, when administered by intravenous infusion, antagonized the decrease in heart rate evoked by serotonin (Bezold-Jarisch reflex) in anaesthetized rats, and the maximal reversal was less than 50%. | [Uses]
GYKI-46903 is a non-competitive antagonist for 5-HT3 receptor, with the pIC50 of 6.91[1]. | [References]
[1] V Csillik-Perczel, et al. GYKI-46 903, a Non-Competitive Antagonist for 5-HT3 Receptors. Comparative Study Pharmacol Toxicol. 1996 Jul;79(1):32-9. DOI:10.1111/j.1600-0773.1996.tb00238.x |
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