Nicardipine HCl is a dihydropyridine that acts as L-type, voltage-gated Ca2+ channel blocker and is used in the clinic to treat hypertension. Nicardipine inhibits L- and T-type CaV channels with similar potency. In human coronary myocytes, nicardipine inhibited the Ca2+ currents with an IC50 of ~2 µM, While in porcine coronary artery strips 2 nM nicardipine were effective in inhibiting the constrictive response to of this muscle to endothelin.
产品描述
A Potent Dihydropyridine Blocker of Ca2+ Channels
产品形式
L-type (CaV1), voltage-gated Ca2+ channels are plasma membrane protein complexes which allow the passage of Ca2+ ions into cells following depolarization of the membrane potential. L-type channels are widely expressed in cardiac and smooth muscle in which they control contraction and therefore were recognized as a therapeutic target for cardiovascular diseases. Dihydropyridines (DHP) are molecules that act as allosteric modulators of L-type channels and many are used in the clinic to treat hypertension.
