Clevidipine-d7 is intended for use as an internal standard for the quantification of clevidipine by GC- or LC-MS. Clevidipine is an inhibitor of L-type calcium channels (IC50s = 7.1 and 78.8 nM at -40 and -80 mV, respectively, in isolated guinea pig cardiomyocytes).1 It preferentially inhibits L-type calcium channels in isolated rat portal vein over rat left ventricle (IC50s = 427 and 20,417 nM, respectively).2 Clevidipine decreases mean arterial pressure in anesthetized normotensive or spontaneously hypertensive rats with ED30 values of 316 and 58 nmol/kg, respectively. Formulations containing clevidipine have been used in the treatment of hypertension.
1.Yi, X., Vivien, B., and Lynch, C., IIIClevidipine blockade of L-type Ca2+ currents: Steady-state and kinetic electrophysiological studies in guinea pig ventricular myocytesJ. Cardiovasc. Pharmacol.36(5)592-600(2000) 2.Norlander, M., SjÖquist, P.O., Ericsson, H., et al.Pharmacodynamic, pharmacokinetic and clinical effects of clevidipine, an ultrashort-acting calcium antagonist for rapid blood pressure controlCardiovasc. Drugs Ther.22(3)227-250(2004)