Tyrosine kinase inhibitors attenuate "capacitative" Ca2+ influx in rat pancreatic acinar cells

Biochem Biophys Res Commun. 1994 Aug 15;202(3):1697-704. doi: 10.1006/bbrc.1994.2130.

Abstract

The effect of several tyrosine kinase inhibitors was tested on Ca2+ influx mediated by thapsigargin-and CCh-induced intracellular store depletion. Genestein inhibited Ca2+ influx in a concentration dependent manner without affecting Ca2+ release or Ca2+ pumping activity. A measureable effect was observed at 3 microM with total inhibition of influx seen at 100 microM. Tyrphostin A25 (300 microM; 78% inhibition) and methyl 2,5 dihydroxycinnamate (10 microM; 51% inhibition) also inhibited Ca2+ influx. The degree of attenuation was not markedly altered by preincubation of the inhibitors. Genestein also inhibited Ca2+ influx induced by CCh. These data indicate that inhibition of Ca2+ influx could in part underlie the previously reported inhibition of enzyme secretion by these agents.

Publication types

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

MeSH terms

  • Animals
  • Barium / metabolism
  • Calcium / metabolism*
  • Carbachol / pharmacology
  • Catechols / pharmacology*
  • Cinnamates / pharmacology*
  • Genistein
  • Ion Transport / drug effects
  • Isoflavones / pharmacology*
  • Male
  • Nitriles / pharmacology*
  • Pancreas / drug effects*
  • Pancreas / metabolism
  • Protein-Tyrosine Kinases / antagonists & inhibitors*
  • Rats
  • Rats, Sprague-Dawley
  • Terpenes / pharmacology
  • Thapsigargin
  • Tyrphostins*

Substances

  • Catechols
  • Cinnamates
  • Isoflavones
  • Nitriles
  • Terpenes
  • Tyrphostins
  • tyrphostin 47
  • Barium
  • methyl 2,5-dihydroxycinnamate
  • Thapsigargin
  • Carbachol
  • Genistein
  • Protein-Tyrosine Kinases
  • Calcium