Abstract

Interaction of σ receptors with intracellular Ca 2+ channel blocker and modulators was examined. Ryanodine and inositol 1,4,5-trisphosphate (IP 3) 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 IP 3 receptor antagonist heparin inhibited [ 3H](+)-SKF-10047 to σ receptors in an uncompetitive manner with a K i of 93 μM. These results suggest that σ receptors may bear some relationship with IP 3 receptor associated proteins or channels.

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