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Alomone Labs Felodipine 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 and 10 μM Felodipine (#F-105) as indicated on the left. Holding potential was -100 mV and currents were elicited every 10 seconds by 100 ms steps to +10 mV.
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. Felodipine is a DHP that acts as L-type, voltage-gated Ca2+ channel blocker and is used in the clinic to treat hypertension2. Felodipine is used as a pharmacological tool to specifically target L-type channels in expression systems3,4 as well as in physiological preparations5. 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 cells5.
Felodipine (#F-105) is a highly pure, synthetic, and biologically active compound.