The imidazoline derivative calmidazolium inhibits voltage-gated Ca2+-channels and insulin release but has no effect on the phospholipase C system in insulin producing RINm5F-cells-Reference-Cited by-同舟云学术

The imidazoline derivative calmidazolium inhibits voltage-gated Ca2+-channels and insulin release but has no effect on the phospholipase C system in insulin producing RINm5F-cells

Published:1994-06-01 Issue:3 Volume:14 Page:145-158
ISSN:0144-8463
Container-title:Bioscience Reports
language:en
Short-container-title:

Author:

Kindmark Henrik¹,Köhler Martin¹,Gerwins Pär²,Larsson Olof¹,Khan Akhtar¹,Wahl Martin A.¹,Berggren Per-Olof²

Affiliation:

1. The Rolf Luft Center for Diabetes Research, Department of Molecular Medicine, Karolinska Institute Karolinska Hospital S-171 76, Stockholm, Sweden

2. Department of Pharmacology, Karolinska Institute, Box 60 400 S-104 01, Stockholm, Sweden

Abstract

The present study shows that the calmodulin antagonist calmidazolium inhibited influx of Ca2+ through voltage-gated Ca2+-channels in clonal insulin producing RINm5F-cells. The mechanism of inhibition may involve both Ca2+-calmodulin-dependent protein kinases and direct binding of calmidazolium to the Ca2+-channel. Calmidazolium did not affect uptake of Ca2+ into intracellular Ca2+-pools, inositol 1,4,5-trisphosphate (InsP3) formation or action on intracellular Ca2+-pools. The calmodulin inhibitor also did not affect glucose utilization or oxidation in RINm5F-cells, speaking against an unspecific toxic effect of the compound. KCl-and ATP-stimulated insulin release from RINm5F-cells was attenuated by calmidazolium, whereas basal hormone secretion was unaffected.

Publisher

Portland Press Ltd.

Subject

Cell Biology,Molecular Biology,Biochemistry,Biophysics

Link

https://portlandpress.com/bioscirep/article-pdf/14/3/145/468919/bsr0140145.pdf

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