Am J Hypertens. 1991 Jul;4(7):422S-429S. doi: 10.1093/ajh/4.7.422s.

Sites, mechanisms of action, and differentiation of calcium channel antagonists.

American journal of hypertension

D J Triggle

PMID: 1654937 DOI: 10.1093/ajh/4.7.422s

Abstract

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.

Substances

• Calcium Channel Blockers
• Calcium Channels
• Receptors, Cell Surface

MeSH terms

• Animals
• Calcium Channel Blockers / chemistry
• Calcium Channel Blockers / pharmacology
• Calcium Channels / metabolism
• Calcium Channels / physiology
• Humans
• Receptors, Cell Surface / metabolism
• Receptors, Cell Surface / physiology

Publication Types

• Journal Article
• Review

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