Dihydropyridine and peripheral type benzodiazepine binding sites: subcellular distribution and molecular size determination

Eur J Pharmacol. 1985 Dec 17;119(3):153-67. doi: 10.1016/0014-2999(85)90291-2.

Abstract

Electrophysiological and pharmacological studies have shown that peripheral-type benzodiazepine receptors modulate voltage-sensitive calcium channels in the heart. We have compared these binding sites with binding sites for [3H]dihydropyridines, which are believed to label such channels. Although no direct or allosteric interaction could be demonstrated between the two sites, their subcellular distribution--sarcolemma and ryanodine-sensitive sarcoplasmic reticulum--was parallel. Size determination of the two sites suggests that the receptors for these two classes of compounds are separate molecules packaged in the same membrane compartment.

MeSH terms

  • Animals
  • Benzodiazepinones / metabolism
  • Benzodiazepinones / pharmacology
  • Binding Sites
  • Calcium / metabolism
  • Calcium Channel Blockers / metabolism*
  • Calcium Channels
  • Cell Fractionation
  • Dogs
  • Ion Channels
  • Isoquinolines / metabolism
  • Isoquinolines / pharmacology
  • Isradipine
  • Male
  • Molecular Weight
  • Myocardium / metabolism
  • Myocardium / ultrastructure*
  • Nifedipine / analogs & derivatives
  • Nifedipine / metabolism
  • Nifedipine / pharmacology
  • Nitrendipine
  • Oxadiazoles / metabolism
  • Rats
  • Rats, Inbred Strains
  • Receptors, GABA-A / metabolism*
  • Receptors, Nicotinic / metabolism*
  • Sarcolemma / metabolism*
  • Sarcoplasmic Reticulum / metabolism*
  • Verapamil / metabolism
  • Verapamil / pharmacology

Substances

  • Benzodiazepinones
  • Calcium Channel Blockers
  • Calcium Channels
  • Ion Channels
  • Isoquinolines
  • Oxadiazoles
  • Receptors, GABA-A
  • Receptors, Nicotinic
  • 4'-chlorodiazepam
  • Nitrendipine
  • Verapamil
  • Nifedipine
  • Calcium
  • PK 11195
  • Isradipine