- Alomone Labs Amlodipine besylate blocks L-type Ca2+ currents in Xenopus oocytes.A. Time course of L-type channel (CaV1.2+α2δ1+β1a) activity before and during applications of 100 μM Amlodipine besylate (#A-120) (green) and upon wash. Holding potential was -100 mV and currents were elicited every 10 seconds by 100 ms steps to 0 mV. B. Example current traces before (black) and during application of 100 μM Amlodipine besylate (taken from the experiment described in A).
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 where they control contraction. Consequently, these channels were recognized as a therapeutic target for cardiovascular diseases1,2.
Dihydropyridines (DHP) are molecules that act as allosteric modulators of L-type channels. Many are used in the clinic to treat hypertension2,3. Amlodipine besylate is a DHP that acts as an L-type, voltage-gated Ca2+ channel blocker and is used in the clinic to treat hypertension3,4. Amlodipine inhibits Ca2+-induced contractions in depolarised rat aorta (IC50 1.9 nM) but displays a very slow action onset. Contractions induced by depolarising steps with 45 mM K+ are far less potently blocked by amlodipine (IC50 19.4 nM) and guinea pig papillary muscle single-cell slow action potentials are blocked at a concentration of 5 mM4. Amlodipine besylate inhibits L- and T-type CaV channels with similar potency5.
Amlodipine besylate (#A-120) is a highly pure, synthetic, and biologically active compound.