- Alomone Labs Nicardipine HCl blocks L-type Ca2+ currents in Xenopus oocytes.Superimposed current traces of L-type channels (CaV1.2+α2δ1+β1a), before and during applications of 1, 10 and 100 μM Nicardipine HCl (#N-125) as indicated on the left. Holding potential was -100 mV and currents were elicited every 10 seconds by 100 ms steps to +10 mV.
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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 diseases1,2. Dihydropyridines (DHP) are molecules that act as allosteric modulators of L-type channels and many are used in the clinic to treat hypertension2.
Nicardipine HCl is a dihydropyridine that acts as L-type, voltage-gated Ca2+ channel blocker and is used in the clinic to treat hypertension3,4. Nicardipine inhibits L- and T-type CaV channels with similar potency5. In human coronary myocytes, nicardipine inhibited the Ca2+ currents with an IC50 of ~2 µM6, While in porcine coronary artery strips 2 nM nicardipine were effective in inhibiting the constrictive response to of this muscle to endothelin7.
Nicardipine HCl (#N-125) is a highly pure, synthetic, and biologically active compound.