Widely used L-type calcium channel blockers (dihydropyridines and phenylalkylamines) also inhibit T-type calcium channels at clinically relevant concentrations, which may contribute to their pharmacological profile.
May contribute to effects of common L-type blockers; leaves open clinical relevance of CaV3 isoform selectivity.
Since cloning of the T-type or Ca(V)3.n calcium channel family in 1998-1999 much progress was made in investigation of their regulation. Most effective metal Ca(V)3 channel blockers are trivalent cations from lanthanide group together with transition metals La(3+) and Y(3+). Divalent cations Zn(2+), Cu(2+) and Ni(2+) inhibit Ca(V)3.2 channels more efficiently than Ca(V)3.1 and Ca(V)3.3 channels via second high-affinity binding site including histidine H191 specific for the Ca(V)3.2 channel. Dihydropyridines and phenylalkylamines in addition to block of L-type calcium channel can inhibit Ca(V)3 channels in clinically relevant concentration.
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Ľubica Lacinová (2011) studied this question.
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