Ivabradine-d3 is intended for use as an internal standard for the quantification of ivabradine by GC- or LC-MS. Ivabradine is a hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker that blocks the mixed sodium/potassium inward funny current (If) in HEK293 cells expressing mouse HCN1, human HCN2, and human HCN4 (EC50s = 4.5, 4.52, and 4.28 μM, respectively).1 In vivo, ivabradine (10 mg/kg per day) reduces heart rate, incidence of ventricular tachycardia and ventricular fibrillation, and arrhythmic mortality in a rat model of myocardial infarction.2 Formulations containing ivabradine have been used in the treatment of heart failure and angina.
1.Melchiorre, M., Del Lungo, M., Guandalini, L., et al.Design, synthesis, and preliminary biological evaluation of new isoform-selective f-current blockersJ. Med. Chem.53(18)6773-6777(2010) 2.Mackiewicz, U., Gerges, J.Y., Chu, S., et al.Ivabradine protects against ventricular arrhythmias in acute myocardial infarction in the ratJ. Cell Physiol.229(6)813-823(2014)