Uses
Nisoldipine-d6 is the deuterium labeled Nisoldipine. Nisoldipine(BAY-k 5552; Sular) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with an IC50 of 10 nM.
Biological Activity
Nisoldipine-d6 is intended for use as an internal standard for the quantification of nisoldipine by GC- or LC-MS. Nisoldipine is a calcium channel inhibitor.1 It binds to calcium channels in isolated rat ventricular membranes (Kd = 0.04 nM) and inhibits calcium uptake by smooth muscle cells.1,2 Nisoldipine inhibits acetylcholine-induced contraction of isolated rabbit coronary arteries (IC50 = 0.03 nM).1 In vivo, nisoldipine (3 mg/kg) reduces ventricular tachycardia and fibrillization and increases survival in a rat model of ventricular arrhythmias induced by myocardial ischemia.3 Dietary administration of nisoldipine (50-100 mg/kg) reduces systolic blood pressure in spontaneously hypertensive rats.4 Formulations containing nisoldipine have been used in the treatment of hypertension.
References
1.Knorr, A.The pharmacology of nisoldipineCardiovasc. Drugs Ther.1(4)393-402(1987)
2.Janis, R.A., Shrikhande, A.V., Greguski, R., et al.Review of nisoldipine binding studiesNisoldipine 198727-35(1987)
3.Fagbemi, O., and Parratt, J.R.Suppression by orally-administered nifedipine, nisoldipine and niludipine of early, life-threatening ventricular arrhythmias resulting from acute myocardial ischaemiaBr. J. Pharmacol.74(1)12-14(1981)
4.Stasch, J.-P., Kazda, S., Hirth, C., et al.Role of nisoldipine on blood pressure, cardiac hypertrophy, and atrial natriuretic peptides in spontaneously hypertensive ratsHypertension10(3)303-307(1987)
