The Ca2+ release activities of D-myo-inositol 1,4,5-trisphosphate analogs are quantized.

Comparison is made between several synthetic stereo and positional isomers of D-myo-inositol 1,4,5-trisphosphate (D-myo-1,4,5-IP3) with respect to their ability to mobilize calcium from the internal stores of saponin-permeabilized rat basophilic leukemia cells. D- and L-myo-Inositol 1,4,5-trisphosphates, D- and L-myo-inositol 2,4,5-trisphosphates, D- and L-chiro-inositol 1,3,4-trisphosphates, D,L-trans-1,2-cyclohexane-diol bisphosphate, D,L-myo-inositol 4,5-bisphosphate, L-glycerol 1,2-bisphosphate, glycerol 1,3-bisphosphate and D,L-(1R,3R,4R)-1-phosphoryloxymethyl-trans-3,4-cyclohexanediol bisphosphate were tested. The analogs, each of which contains a vicinal trans-1,2-diol-bisphosphate motif, displayed potencies that were distributed over a 10(4)-fold range of concentration and fell into 4 distinct classes of activity.