RG-12915

RG-12915 is a selective 5-HT3 antagonist, with IC₅₀ value of 0.16 nM. IC50 & Target:IC50: 0.16 nM (5-HT3)^[1] In Vitro: RG 12915 is a potent and selective displacer of binding of 5-hydroxytryptamine (5-HT3) binding sites (IC₅₀ value = 0.16 nM), whereas failing to displace binding of ligands for the alpha-1, alpha-2 and beta adrenergic, 5-HT1 or 5-HT2 or cholinergic-muscarinic sites with IC₅₀ values less than 1 μM. In Vivo: RG 12915 has a lower ED₅₀ value (0.004 mg/kg) for attenuating cisplatin-induced emetic episodes in the ferret. RG 12915 (1 mg/kg, p.o.) is highly protective against cisplatin-induced emesis in the dog. RG 12915 has no significant gastroprokinetic activity in the same species^[1].