Manidipine inhibits endothelin-1-induced [Ca2+]i signaling but potentiates endothelin's effect on c-fos and c-jun induction in vascular smooth muscle and glomerular mesangial cells

Am Heart J. 1993 Feb;125(2 Pt 2):589-97. doi: 10.1016/0002-8703(93)90208-q.

Abstract

We studied the effects of manidipine, a newly synthesized dihydropyridine Ca2+ channel antagonist, on endothelin-1 (ET-1)-induced [Ca2+]i signaling and immediate-early gene induction in vascular smooth muscle A7r5 cells and glomerular mesangial cells (MCs). ET-1-induced a dose-dependent, biphasic increase in [Ca2+]i in both A7r5 cells and MCs. Manidipine inhibited the ET-1-induced [Ca2+]i increase by reducing both the transient and sustained Ca2+ increments in A7r5 cells and MCs. At concentrations of 10(-10) to 10(-6) mol/L, inhibition was dose dependent with a median effective dose (ED50) of 10(-9) mol/L. A 20-minute preincubation period was required to observe the maximal inhibitory effect of manidipine. In contrast, manidipine (10(-5) mol/L) potentiated ET-1-induced c-fos and c-jun expression in A7r5 cells. This potentiating effect appeared 30 minutes after manidipine was added to the media and lasted for 15 hours. Manidipine alone had no detectable effect on c-fos steady-state messenger ribonucleic acid level. Manidipine induced c-jun expression starting at 60 minutes but with much lower potency. These data demonstrate that manidipine is a potent inhibitor for ET-1-induced [Ca2+]i signaling and that manidipine has multiple effects on ET-1-induced signaling, including potentiating the immediate-early gene response.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Calcium / metabolism
  • Calcium / physiology*
  • Calcium Channel Blockers / pharmacology*
  • Calcium Channels / drug effects
  • Cell Line
  • Cells, Cultured
  • Dihydropyridines / pharmacology*
  • Dose-Response Relationship, Drug
  • Endothelins / physiology*
  • Gene Expression Regulation / drug effects
  • Genes, fos / drug effects
  • Genes, jun / drug effects
  • Glomerular Mesangium / cytology
  • Glomerular Mesangium / drug effects*
  • Male
  • Muscle, Smooth, Vascular / cytology
  • Muscle, Smooth, Vascular / drug effects*
  • Nitrobenzenes
  • Piperazines
  • Proto-Oncogenes / drug effects*
  • Rats
  • Signal Transduction / drug effects
  • Transcriptional Activation

Substances

  • Calcium Channel Blockers
  • Calcium Channels
  • Dihydropyridines
  • Endothelins
  • Nitrobenzenes
  • Piperazines
  • manidipine
  • Calcium