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 V
Conivaptan, a non-peptide inhibitor of antidiuretic hormone, was approved for hyponatremia caused by the syndrome of inappropriate antidiuretic hormone (SIADH), there is also some evidence that it may be effective in heart failure. Conivaptan inhibits sub
L-368899 is a non-peptide and orally active antagonist of oxytocin receptor (IC50: 8.9 nM). It displays 40-fold selectivity over vasopressinV1a and V2 receptors (IC50: 370 and 570 nM respectively).
Selective vasopressin V1B receptor agonist (Ki values are 0.16, 64, 100 and 3800 nM for V1B, oxytocin, V2 and V1Areceptors respectively). Displays weak antidiuretic, vasopressor and in vitro oxytocic activities.
Potent and selective human vasopressin V1B receptor agonist (Ki values are 1.2, 151, 240 and 750 nM for V1B, V1A, Oxytocin and V2 receptors respectively). Stimulates ACTH and corticosterone secretion and exhibits negligible vasopressor activity in vivo.
Selective vasopressinV1Areceptor antagonist. Inhibits vasopressin and oxytocin-induced increases in intracellular calcium concentrations in vitro (IC50 values are 5 and 30 nM respectively). Exhibits potent and prolonged antivasopressor activity and indu