Calcium channel agonist and antagonist effects of the stereoisomers of the dihydropyridine 202-791

Sathapana Kongsamut*, Timothy J. Kamp, Richard J. Miller, Michael C. Sanguinetti

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

40 Scopus citations

Abstract

The effects of the pure stereoisomers of the novel dihydropyridine 202-791 on voltage sensitive calcium channels in nerve and cardiac muscle were examined. The (-)-isomer blocked depolarization-induced uptake of 45Ca2+ into NG108-15 neuroblastoma x glioma cells, blocked the depolarization-induced release of [3H]-norepinephrine from PC12 cells and reduced the Vmax of the slow response action potential recorded from guinea pig papillary muscle. In contrast, the (+)-isomer enhanced these same processes. In papillary muscle, greater enhancement of the slow responses was observed at lower stimulation frequencies. Thus, the (-) and (+) stereoisomers of 202-791 can be shown to be calcium channel antagonist and agonist respectively.

Original languageEnglish (US)
Pages (from-to)141-148
Number of pages8
JournalBiochemical and Biophysical Research Communications
Volume130
Issue number1
DOIs
StatePublished - Jul 16 1985

ASJC Scopus subject areas

  • Biophysics
  • Biochemistry
  • Molecular Biology
  • Cell Biology

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