Sites, mechanisms of action, and differentiation of calcium channel antagonists.
The calcium channel antagonists are a chemically heterogeneous group of agents that includes verapamil, nifedipine, and diltiazem as first-generation agents. They owe their effectiveness to interactions at specific sites associated with a major protein of the L class of voltage-gated channel. The calcium channel may be viewed as a pharmacologic receptor, with specific sites for activator and antagonist ligands that are linked to the functional machinery of the channel. These sites are subject to homologous and heterologous regulation and a number of disease states--both experimental and clinical--alter their expression. The selective actions of these agents are reviewed from several perspectives, particularly that of voltage-dependent interactions that distinguish between cells according to membrane potential and other factors.
Triggle
D J
DJ
School of Pharmacy, State University of New York, Buffalo 14260.
D000818:Animals; D002121:Calcium Channel Blockers / Q000737:chemistry / Q000494:pharmacology*; D015220:Calcium Channels / Q000378:metabolism / Q000502:physiology; D006801:Humans; D011956:Receptors, Cell Surface / Q000378:metabolism / Q000502:physiology
D002121:Calcium Channel Blockers; D015220:Calcium Channels; D011956:Receptors, Cell Surface