Description
A 5-HT3 receptor antagonist (Ki = 20 nM); selective for 5-HT3 receptors over 5-HT1A, 5-HT1B, 5-HT2, dopamine D2, α1-, α2-, β-adrenergic, M1-5 muscarinic acetylcholine, and NK1 receptors (IC50s = >10 µM for all); inhibits 5-HT-induced membrane currents in NG 108-15 cells (IC50 = 3.8 nM); increases the latency to emesis and reduces the number of vomiting and retching episodes induced by cisplatin in ferrets at 0.5 or 2 mg/kg