Calcium channels and calcium channel drugs: recent biochemical and biophysical findings

Arzneimittelforschung. 1985;35(12A):1917-35.

Abstract

The biochemical and biophysical features of the voltage-dependent calcium channels, as discovered in vitro by means of radiolabelled drugs, are presented. The concept of distinct but reciprocally allosterically coupled drug receptor domains linked to calcium binding sites is explained. The evidence for the existence of isochannels (and isoreceptors) is reviewed and the voltage-dependence of 1,4-dihydropyridine binding and action is discussed. The structure of the channel is investigated by radiation-inactivation and by photoaffinity labelling. Low affinity binding sites for calcium channel drugs are shown to reside on the nucleoside carrier.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Adenosine / metabolism
  • Affinity Labels
  • Animals
  • Autoradiography
  • Buffers
  • Calcium Channel Blockers / pharmacology*
  • Dihydropyridines*
  • Erythrocyte Membrane / metabolism
  • Humans
  • Indicators and Reagents
  • Ion Channels / drug effects*
  • Ion Channels / metabolism
  • Photochemistry
  • Pyridines / metabolism

Substances

  • Affinity Labels
  • Buffers
  • Calcium Channel Blockers
  • Dihydropyridines
  • Indicators and Reagents
  • Ion Channels
  • Pyridines
  • 1,4-dihydropyridine
  • Adenosine