Abstract

Neoplastic rat liver epithelial (261B) cells made permeable by electroporation released 0.2-0.3 μM Ca 2+ from intracellular stores in response to 0.5 μM Ins(1,4,5)P 3 stimulation. This Ca 2+ release response was found to be inhibited by heparin in a dose-dependent manner (K i of 15 μg/ml). Two other glycosaminoglycans, chondroitin sulfate and hyaluronic acid, showed no inhibitory effect at doses as high as 0.2 mg/ml. Passive Ca 2+ release, and sequestration of Ca 2+ into intracellular storage sites by the action of Ca 2+-ATPase were unaffected by heparin treatment. We conclude that the inhibitory action of heparin treatment on Ca 2+ mobilization in permeabilized 261B cells is mediated through its interaction at the Ins(1,4,5)P 3 receptor binding site.

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