Recent development in calcium channel antagonists.

D J Triggle; R A Janis

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PubMed · 2559260

Recent development in calcium channel antagonists.

D J Triggle·R A Janis

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Abstract

The introduction of the Ca2+ channel antagonists, including the clinically available verapamil, nifedipine and diltiazem, into cardiovascular medicine served to initiate much work directed to the elucidation of their mechanisms of action at voltage-dependent Ca2+ channels. The Ca2+ channel ligands (both activator and antagonist) interact with the channel in a state-dependent manner associating preferentially with open states (activators) or open and inactivated states (antagonists). Both frequency- and voltage-dependent interactions occur with activator and antagonist drugs. These effects underlie the antiarrhythmic activity of verapamil and the vascular smooth muscle selectivity of 1,4-dihydropyridines. Selectivity of action occurs from a combination of factors including the relative Ca2+ demands of the system, the stimulus mode and state dependence of interaction, the agonist/antagonist character of the channel ligand and the category of Ca2+ channel involved.

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Animals Calcium Channel Blockers Calcium Channels Structure-Activity Relationship Journal Article Research Support, U.S. Gov't, P.H.S.Review

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D J Triggle, R A Janis. 1989. Recent development in calcium channel antagonists.. https://pubmed.ncbi.nlm.nih.gov/2559260/

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