Calcium Uptake Inhibition Activity

  • Michael Gralinski
  • Liomar A. A. Neves
  • Olga Tiniakova
Living reference work entry

Abstract

Cellular calcium flux is regulated by receptor-operated and voltage-dependent channels, which are sensitive to inhibition by calcium entry blockers. The term calcium antagonist was introduced by Fleckenstein (1964, 1967) when two drugs, prenylamine and verapamil, originally found as coronary dilators in the Langendorff experiment, were shown to mimic the cardiac effects of simple Ca2+ withdrawal, diminishing Ca2+-dependent high-energy phosphate utilization, contractile force, and oxygen requirement of the beating heart without impairing the Na+-dependent action potential parameters. These effects were clearly distinguishable from β-receptor blockade and could promptly be neutralized by elevated Ca2+, β-adrenergic catecholamines, or cardiac glycosides, measures that restore the Ca2+ supply to the contractile system. In the following years, many Ca2+ antagonists were introduced to therapy. Specific Ca2+ antagonists interfere with the uptake of Ca2+ into the myocardium and prevent myocardial necrotization arising from deleterious intracellular Ca2+ overload. They act basically as specific inhibitors of the slow transsarcolemnal Ca2+ influx but do not or only slightly affect the fast Na+ current that initiates normal myocardial excitation.

Keywords

Calcium Channel Calcium Antagonist Calcium Channel Antagonist Calcium Entry Blocker Intracellular Action Potential 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

References and Further Reading

General Considerations

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Calcium Antagonism in the Isolated Guinea Pig Pulmonary Artery

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In Vivo Methods

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Copyright information

© Springer-Verlag Berlin Heidelberg 2015

Authors and Affiliations

  • Michael Gralinski
    • 1
  • Liomar A. A. Neves
    • 1
  • Olga Tiniakova
    • 1
  1. 1.CorDynamics, Inc.ChicagoUSA

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