Rapid communicationIP3 receptor antagonist heparin uncompetitively inhibits [3H](+)-SKF-10047 (cas 133005-41-1) binding to σ receptors

Add time:08/31/2019    Source:sciencedirect.com

Interaction of σ receptors with intracellular Ca2+ channel blocker and modulators was examined. Ryanodine and inositol 1,4,5-trisphosphate (IP3) did not inhibit [3H](+)-N-allylnormetazocine ([3H](+)-SKF-10047) binding to σ receptors from either brain microsomal fractions or liver membrane extracts of the rat. However, the IP3 receptor antagonist heparin inhibited [3H](+)-SKF-10047 to σ receptors in an uncompetitive manner with a Ki of 93 μM. These results suggest that σ receptors may bear some relationship with IP3 receptor associated proteins or channels.

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