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Tolvaptan is a nonpeptide vasopressin V2 receptor antagonist (IC50 = 3 nM for rat receptor) and a diuretic agent.1 It is selective for V2 over V1 receptors (IC50 = 0.58 μM). Tolvaptan increases urine volume by 3-fold in rats when administered at a dose of 0.54 mg/kg. It also reduces left ventricular end-systolic volumes and improves left ventricular ejection fraction in a rat model of myocardial infarction.2 Formulations containing tolvaptan have been used to treat hyponatremia.
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