Different modes of Ca channel gating behaviour favoured by dihydropyridine Ca agonists and antagonists

Nature. 1984 Oct 11-17;311(5986):538-44. doi: 10.1038/311538a0.

Abstract

Single cardiac transmembranous Ca channels have three modes of gating behaviour in the absence of drugs, expressed as current records with brief openings (mode 1), with no openings because of channel unavailability (mode 0 or null mode) and with long-lasting openings and very brief closings that appear only rarely (mode 2). The dihydropyridine Ca agonist Bay K 8644 enhances Ca channel current by promoting mode 2, while the Ca antagonists nitrendipine and nimodipine inhibit the current by favouring mode 0.

Publication types

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

MeSH terms

  • 3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)-, Methyl ester
  • Animals
  • Calcium / physiology*
  • Calcium Channel Blockers / pharmacology*
  • Electric Conductivity / drug effects
  • Guinea Pigs
  • Heart / physiology
  • Ion Channels / drug effects*
  • Kinetics
  • Nicotinic Acids / pharmacology
  • Nifedipine / analogs & derivatives
  • Nifedipine / pharmacology
  • Nimodipine
  • Nitrendipine
  • Ranidae
  • Sarcolemma / physiology*
  • Structure-Activity Relationship

Substances

  • Calcium Channel Blockers
  • Ion Channels
  • Nicotinic Acids
  • Nimodipine
  • 3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)-, Methyl ester
  • Nitrendipine
  • Nifedipine
  • Calcium