Table 1. Inhibition of multiple hTAS2Rs by GIV3727.
| Receptor | Bitter Agonist | % activation in presence of GIV3727 |
p-value |
|---|---|---|---|
| hTAS2R1 | 30 μM trans-isohumulone | 114.3 ± 6.2% | 0.2268 |
| hTAS2R3 | 3 mM chloroquine | 76.7 ± 21.5% | 0.2762 |
| hTAS2R4 | 10 mM colchicine | 45.8 ± 17.4% | 0.0067 |
| hTAS2R5 | 300 μM phenanthrolin | 100.2 ± 56.9% | 0.9954 |
| hTAS2R7 | 10 mM cromolyn | 47.8 ± 17.0% | 0.0004 |
| hTAS2R8 | 100 μM chloramphenicol | 95.7 ± 30.6% | 0.8422 |
| hTAS2R10 | 100 μM strychnine | 93.9 ± 16.4% | 0.4598 |
| hTAS2R13 | 3 mM denatonium benzoate | 97.5 ± 15.1% | 0.7814 |
| hTAS2R14 | 3 μM aristolochic acid | 94.3 ± 14.8% | 0.618 |
| hTAS2R16 | 10 mM salicin | 101.1 ± 13.5% | 0.8977 |
| hTAS2R38 | 10 μM PTC | 104.0 ± 14.6% | 0.5599 |
| hTAS2R39 | 100 μM EGCG | 93.7% ± 12.8% | 0.6043 |
| hTAS2R40 | 0.3 μM cohumulone | 3.2 ± 6.5% | 9.1×10−6 |
| hTAS2R43 | 0.3 μM aristolochic acid | 2.5 ± 4.9% | 1.4×10−7 |
| hTAS2R31 | 3 μM aristolochic acid | 61.9 ± 9.3% | 0.0013 |
| hTAS2R46 | 3 μM strychnine | 92.6 ± 8.9% | 0.1571 |
| hTAS2R20 | 100 μM cromolyn | 62.9 ± 31.8% | 0.034 |
| hTAS2R50 | 300 μM andrographolide | 119.0 ± 14.2% | 0.0263 |
Data are presented as the mean ± s.e.m. of n=3 experiments and have been expressed as a percent of the signal obtained with agonist in the absence of inhibitor. Statistical significance was assessed by student’s t-test and p < 0.05 is considered statistically significant. Abbreviations; phenythiocarbamide (PTC), epigallocatechin gallate (EGCG). See also Figure S2.