Table 1.
Biochemical, biological and physiological features of sweet tasting compounds.
| Kd (µM) | EC50 (µM) | Relative sweetness | |||
|---|---|---|---|---|---|
| hTAS1R2 | hTAS1R2/hTAS1R3 | hTAS1R2 | hTAS1R3 | ||
| Neotame | 2.78 ± 0.69 | 0.90 ± 0.09 | n.r. | n.r. | 11,000 |
| Perillartine | 373 ± 110 | 2.54 ± 0.48 | 61 ± 13 | n.r. | 2000 |
| Sucralose | 29 ± 8 | 36 ± 2 | n.r. | n.r. | 600 |
| Acesulfame-K | 164 ± 53 | 213 ± 59 | n.r. | n.r. | 200 |
| Cyclamate-Na | n.b. | 767 ± 83 | n.r. | n.r. | 30–50 |
Kd values were determined by intrinsic tryptophan fluorescence. EC50 values were calculated from the ligand dose–response relationship in HEK293T-Gα16gust44 cells transiently transfected with plasmid encoding pGP-CMV-GCaMP6S (fluorescent calcium biosensor), hTAS1R2-FLAG and/or hTAS1R3-FLAG. The relative sweetness of each sweetener is described on a molar basis.
n.r. = no response; n.b. no binding.