SRX246

SRX246 is a potent, BBB-penetrant, highly selective vasopressin 1a (V1a) receptor antagonist (K_i=0.3 nM for human V1a). SRX246 has no interaction at V1b and V2 receptors. SRX246 also displays negligible binding at 64 others receptors classes, including 35 G-proteincoupled receptors. SRX246 can be used for treatment of stress-related disorders^[1]. IC50 & Target:Ki: 0.3 nM (human vasopressin 1a receptor)^[1] In Vivo:SRX246 (2 mg/kg; i.v.) treatment shows that the C_max, AUC_0-∞ and t_1/2 values are 953 ng/mL, 1141 ng h/mL, and 6.02 hours, respectively, in plasma pharmacokinetics. Following an oral administration (dose 20 mg/kg), The C_max, AUC_0-∞ and t_1/2 values are 98.4 ng/mL, 624 ng h/mL and 2.38 hours, respectively^[1].