RG-12915 is a selective antagonist of 5-HT3(IC50 value of 0.16 nM).

5-HT3:0.16 nM

RG 12915 is a displacer of binding of 5-hydroxytryptamine (5-HT3) binding sites with IC50 value of 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 (IC50 values less than 1 μM).

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. RG 12915 has a lower ED50 value for attenuating cisplatin-induced emetic episodes in the ferret[1].