Tolvaptan-d7 is intended for use as an internal standard for the quantification of tolvaptan by GC- or LC-MS. 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.
1.Kondo, K., Ogawa, H., Yamashita, H., et al.7-Chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoyl-amino)benzoyl ]-2,3,4,5-tetrahydro-1H-1-benzazepine (OPC-41061): A potent, orally active nonpeptide arginine vasopressin V2 receptor antagonistBioorg. Med. Chem.7(8)1743-1754(1999) 2.Yamazaki, T., Nakamura, Y., Shiota, M., et al.Tolvaptan attenuates left ventricular fibrosis after acute myocardial infarction in ratsJ. Pharmacol. Sci.123(1)58-66(2013)