Description
A nonpeptide antagonist of vasopressin V1 receptors (IC50 = 0.4 µM in rat liver membranes); selective for V1 over V2 receptors (IC50 = >100 µM in kidney membranes); selective for rat over human V1 receptors (Kis = 25 and 8,800 nM, respectively); inhibits pressor responses induced by arginine vasopressin in pithed rats at 0.03-1 mg/kg; inhibits arginine vasopressin-induced vasoconstriction in conscious rats (ID50 = 2 mg/kg); induces hypotension in aged SHRs and stroke-prone SHRs at 3 mg/kg