SRX246 has no interaction at V1b and V2 receptors. SRX246 shows negligible binding at 64 other receptors classes, including 35 G-proteincoupled receptors. SRX246 is a potent and CNS-penetrant vasopressin 1a (V1a) receptor antagonist (Ki=0.3 nM for human V1a).

SRX246 (2 mg/kg; i.v.) treatment shows that the Cmax, AUC0-∞ and t1/2 values are 953 ng/mL, 1141 ng ?h/mL, and 6.02 hours, respectively, in plasma pharmacokinetics. SRX246 (20 mg/kg; p.o.) administration display that the Cmax, AUC0-∞ and t1/2 values are 98.4 ng/mL, 624 ng ?h/mL and 2.38 hours, respectively [1].

512784-93-9

C42H49N5O5

703.87

SRX246

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years