Abstract
The Ca2+ channel blockers represent a successful group of therapeutic agents directed against cardiovascular targets, including hypertension and angina. These drugs, including the first-generation verapamil, nifedipine and diltiazem are directed against a subclass of voltage-gated Ca2+ channel - the L-type channel. Other subclasses of Ca2+ channel exist and are targets for new indications. The mechanisms of actions of the L-type blockers are discussed and the origins of their cardiovascular selectivity discussed. Although new drugs of this class directed against hypertension could be developed, there are both clinical and economic reasons that argue against such development. However, there are other possible targets to investigate where antagonists and activators of the L-type channel may be useful: such targets include fertility, neuronal growth, bone formation and epilepsy. Limitations to these approaches are discussed.
Keywords: Ca2+ channels, Ca2+ channel blockers, hypertension, angina, arrhythmias, neuronal Ca2+ channels, verapamil, diltiazem, nifedipine, 1, 4-dihydropyridines
Current Pharmaceutical Design
Title: L-Type Calcium Channels
Volume: 12 Issue: 4
Author(s): David J. Triggle
Affiliation:
Keywords: Ca2+ channels, Ca2+ channel blockers, hypertension, angina, arrhythmias, neuronal Ca2+ channels, verapamil, diltiazem, nifedipine, 1, 4-dihydropyridines
Abstract: The Ca2+ channel blockers represent a successful group of therapeutic agents directed against cardiovascular targets, including hypertension and angina. These drugs, including the first-generation verapamil, nifedipine and diltiazem are directed against a subclass of voltage-gated Ca2+ channel - the L-type channel. Other subclasses of Ca2+ channel exist and are targets for new indications. The mechanisms of actions of the L-type blockers are discussed and the origins of their cardiovascular selectivity discussed. Although new drugs of this class directed against hypertension could be developed, there are both clinical and economic reasons that argue against such development. However, there are other possible targets to investigate where antagonists and activators of the L-type channel may be useful: such targets include fertility, neuronal growth, bone formation and epilepsy. Limitations to these approaches are discussed.
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Cite this article as:
Triggle J. David, L-Type Calcium Channels, Current Pharmaceutical Design 2006; 12 (4) . https://dx.doi.org/10.2174/138161206775474503
DOI https://dx.doi.org/10.2174/138161206775474503 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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