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Ca2+ Channel Blockers

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Encyclopedia of Molecular Pharmacology

Synonyms

Ca2+ antagonists; Ca2+ channel antagonists

Definition

Ca2+ is an important intracellular second messenger that controls several cellular functions including muscle contraction in smooth and cardiac muscle. Ca2+ channel blockers (“Ca2+ antagonists”) inhibit depolarization-induced Ca2+ entry through one specific member of the voltage-gated Ca2+ channel family, so-called L-type channels. Inhibition of L-type channels in muscle cells of the cardiovascular system causes a decrease in blood pressure, a reduction of cardiac contractility, and has antiarrhythmic effects. Therefore, these drugs are used clinically to treat hypertension, myocardial ischemia, and cardiac arrhythmias.

Mechanism of Action

Voltage-gated Ca2+ channels are Ca2+-selective pores in the plasma membrane of all electrically excitable cells, such as muscle cells, neurons, endocrine cells, and sensory cells. They open in response to membrane depolarization (e.g., an action potential) and permit the influx of Ca2+...

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References

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Author information

Authors and Affiliations

  1. Institut für Pharmazie, Abteilung Pharmakologie und Toxikologie, Center for Molecular Biosciences, Leopold-Franzens-Universität Innsbruck, Innsbruck, Austria

    Jörg Striessnig & Nadine J. Ortner

Authors
  1. Jörg Striessnig
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  2. Nadine J. Ortner
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Corresponding author

Correspondence to Jörg Striessnig .

Editor information

Editors and Affiliations

  1. Max-Planck-Institut Herz/Lungenforschg., Bad Nauheim, Hessen, Germany

    Stefan Offermanns

  2. Presidential Office, Friedrich-Schiller University Jena, Jena, Thüringen, Germany

    Walter Rosenthal

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Striessnig, J., Ortner, N.J. (2020). Ca2+ Channel Blockers. In: Offermanns, S., Rosenthal, W. (eds) Encyclopedia of Molecular Pharmacology. Springer, Cham. https://doi.org/10.1007/978-3-030-21573-6_34-1

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  • DOI: https://doi.org/10.1007/978-3-030-21573-6_34-1

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  • Publisher Name: Springer, Cham

  • Print ISBN: 978-3-030-21573-6

  • Online ISBN: 978-3-030-21573-6

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