| Title
| - Synthesis, Calcium Mobilizing, and Physicochemical Properties ofd-chiro-Inositol 1,3,4,6-Tetrakisphosphate, a Novel and Potent Ligand at thed-myo-Inositol 1,4,5-Trisphosphate Receptor
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| Abstract
| - The synthesis of a novel and potent ligand at the d-myo-inositol 1,4,5-trisphosphate receptor(InsP3R) is described. d-chiro-Inositol 1,3,4,6-tetrakisphosphate (7) and l-chiro-inositol 1,3,4,6-tetrakisphosphate (ent-7) have been synthesized from d-2,5-di-O-benzyl-chiro-inositol and l-2,5-di-O-benzyl-chiro-inositol, respectively. The potency of binding and Ca2+ release of 7 and ent-7were examined in L15 and Lvec cells. 7 was a full agonist at the InsP3R in both cells, andent-7 was inactive. The results are compared to those from d-myo-inositol 1,4,5-trisphosphate(1), dl-scyllo-inositol 1,2,4-trisphosphate (2), dl-myo-inositol 1,2,4,5-tetrakisphosphate (3), scyllo-inositol 1,2,4,5-tetrakisphosphate (4), d-myo-inositol 2,4,5-trisphosphate (5), and d-chiro-inositol1,3,4-trisphosphate (6). The protonation processes of 7 have also been investigated by 31P NMRtitration experiments.
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