WAY-151932 is a vasopressin V2-receptor agonist with IC50 of 80.3 nM and 778 nM in human-V2 binding and V1a binding assay.
WAY-151932 (VNA-932) stimulates cAMP formation in LV2 cells expressing the hV2 receptors in a dose-dependent manner with an EC50 of 0.74±0.07 nM[2].
Oral administration of WAY-151932 (VNA-932) to water-loaded conscious rats produces a dose-dependent decrease in urine volume (ED50=0.14 mg/kg, 2.5% starch in water vehicle) and a corresponding increase in osmolality without altering the urine electrolyte excretion profile[2].
[1]. Molinari AJ, et al. Identification and synthesis of major metabolites of Vasopressin V2-receptor agonist WAY-151932, and antagonist, Lixivaptan. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5796-800. [2]. Failli AA, et al. Pyridobenzodiazepines: a novel class of orally active, vasopressin V2 receptor selective agonists. Bioorg Med Chem Lett. 2006 Feb 15;16(4):954-9.