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L-type (Ca_V1), 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 acts as allosteric modulators of L-type channels and many are used in the clinic to treat hypertension. Amlodipine besylate is a DHP that acts as a L-type, voltage-gated Ca²⁺ channel blocker and is used in the clinic to treat hypertension. Amlodipine inhibit Ca²⁺ -induced contractions in depolarised rat aorta (IC₅₀ 1.9 nM) but, displayes a very slow onset of action. Contractions induced by depolarising steps with 45 mM K⁺ are much 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 Ca_V channels with similar potency.