Felodipine. A Potent and Selective L-Type�Ca2+ Channel Inhibitor.
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. Felodipine is a DHP that acts as L-type, voltage-gated Ca2+ channel blocker and is used in the clinic to treat hypertension.
Felodipine is used as a pharmacological tool to specifically target L-type channels in expression systems as well as in physiological preparations.
The effective concentration of felodipine varies between systems for example; it is higher for inhibition of smooth muscle high K\+\ induced contraction than for inhibition of the intracellular Ca2+ elevation in these cells.
Ion Channel Modulator; Voltage - Gated Ca2+ Channel Blockers