RG-12915 

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

360.88

C₂₀H₂₅ClN₂O₂

136174-04-4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]