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. 2013 Jan 25;8(1):e54877. doi: 10.1371/journal.pone.0054877

Table 2. Relative potencies of IP3 analogues at different IP3 receptor subtypes.

IP3R1 IP3R2 IP3R3
ΔpEC50 Δmax (%) (1,4,5)IP3max (%) ΔpEC50 Δmax (%) (1,4,5)IP3max (%) ΔpEC50 Δmax (%) (1,4,5)IP3max (%)
(4,5)IP2 1.92±0.15 13±5 81±3 1.92±0.05 8±3 65±4 1.38±0.06* −1±2 77±4
2-deoxy(1,4,5)IP3 0.09±0.10 −1±2 81±3 0.19±0.14 −3±3 63±4 −0.17±0.08 0±2 77±4
(1,4,6)IP3 1.57±0.09 −2±5 76±5 1.67±0.15 −3±6 64±5 1.45±0.09 8±6 55±7
3-deoxy(1,4,5)IP3 1.61±0.12 21±2* 80±4 1.64±0.21 12±4* 68±3 1.66±0.17 20±5* 66±3
(1,3,4,5)IP4 a 2.09±0.07 17±5a 77±1 2.18±0.04 7±0* 67±6 2.38±0.07 NDa 77±4
MG(1,4,5)IP3 0.69±0.10 4±5 77±3 0.7±0.14 11±3* 64±3 0.64±0.15 4±4 61±3

From paired comparisons with (1,4,5)IP3, the relative potency Inline graphic and differences in maximal Ca2+ release Inline graphic are shown for each analogue at each IP3R subtype. Results show means ± SEM, with n provided in Table 1. To allow direct comparison with responses evoked by (1,4,5)IP3, maximal Ca2+ release evoked by (1,4,5)IP3 in experiments paired with the analogues are also shown ((1,4,5)IP3 max).

a

With (1,3,4,5)IP4 it was impossible to attain concentrations (>100 µM) that evoked a maximal response for all IP3R subtypes; in these cases the maximal responses were not subject to statistical analysis. The relative potency of (1,3,4,5)IP4 at IP3R subtypes was estimated by assuming it was a full agonist that released the same fraction of the intracellular Ca2+ stores as a maximally effective concentration of (1,4,5)IP3 in parallel analyses. ND, not determined.

*

Denotes values significantly different (P<0.05) from IP3R1 (for ΔpEC50 values) or from (1,4,5)IP3 in paired comparisons with the analogue (for Δmax values).