Molecular Formula | C20H25ClN2O2 |
Molar Mass | 360.88 |
Density | 1.31±0.1 g/cm3(Predicted) |
Boling Point | 462.6±45.0 °C(Predicted) |
pKa | 13.83±0.20(Predicted) |
Storage Condition | Room Temprature |
In vitro study | RG 12915 is a potent and selective displacer of binding of 5-hydroxytryptamine (5-HT3) binding sites (IC 50 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 IC 50 values less than 1 μM. |
In vivo study | RG 12915 has a lower ED 50 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. |
biological activity | RG-12915 is a selective 5-HT3 antagonist with an IC50 value of 0.16 nM. |