RG-12915是一种选择性的5-HT3拮抗剂，IC50值为0.16nM。
CAS：136174-04-4
分子式：C20H25ClN2O2
分子量：360.88
纯度：98%
存储：Store at -20°C

Background:

RG-12915 is a selective 5-HT3 antagonist, with IC50 value of 0.16 nM.

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.

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].

[1]. Fitzpatrick LR, et al. RG 12915: a potent 5-hydroxytryptamine-3 antagonist that is an orally effective inhibitor of cytotoxic drug-induced emesis in the ferret and dog. J Pharmacol Exp Ther. 1990 Aug;254(2):450-5.