Diltiazem enhancement of [3H]nitrendipine binding to calcium channel associated drug receptor sites in rat brain synaptosomes

Henry I. Yamamura, Hans Schoemaker, Richard G. Boles, William R. Roeske

Research output: Contribution to journalArticle

80 Scopus citations

Abstract

The binding of the dihydropyridine calcium channel antagonist [3H]nitrendipine to whole rat brain synaptosomes was studied. Binding was specific, saturable, and of high affinity (Kd = 170 pM). The calcium channel antagonist diltiazem enhanced [3H]nitrendipine binding in synaptosomes in concentrations of 1 and 10 μM. Equilibrium saturation analysis demonstrated that this effect was mediated by a decrease in the dissociation constant, due to a 3-fold reduction in the rate of ligand-receptor complex dissociation. It is concluded that diltiazem allosterically modulates the calcium channel drug receptor labeled by [3H]nitrendipine in this preparation.

Original languageEnglish (US)
Pages (from-to)640-646
Number of pages7
JournalBiochemical and Biophysical Research Communications
Volume108
Issue number2
DOIs
StatePublished - Sep 30 1982

ASJC Scopus subject areas

  • Biophysics
  • Biochemistry
  • Molecular Biology
  • Cell Biology

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