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Development of inositol-based antagonists for thed-myo-inositol 1,4,5-trisphosphate receptor

This paper is available in a repository.
This paper is available in a repository.

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Abstract

The syntheses of four D-myo-inositol 1,4,5-trisphosphate (InsP(3)) derivatives, incorporating phosphate bioisosteres at the 5-position, are reported. The methyl phosphate ester and sulfate derivatives retain InsP(3) receptor (InsP(3)R) agonist activity; the compounds that possess a methylphosphonate or a carboxymethyl moiety are InsP(3)R antagonists.