Table 2.
Pharmacological data for tested compounds (antagonists retrieved within this study) and the reference agonists FFA and aristolochic acid obtained by measuring Gαqi-mediated accumulation of IPa1
| Agonistic effect | Inhibitory effectb | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| EC50 (µM)c | Emax (%)d | nf | FFA as agonist | Aristolochic acid as agonist | |||||
| IC50 (µM)f | Emax (%)g | Ne | IC50 (µM)h | Emax (%)g | Ne | ||||
| FFA | 0.43 ± 0.04 | 100 | 10 | – | – | – | – | – | – |
| Aristol. acid | 0.83 ± 0.2 | 100 | 4 | – | – | – | – | – | – |
| LW 118 | – | < 5 | 2 | 4.0 ± 0.49 | 83 ± 4 | 8 | 2.7 ± 4.1 | 82 ± 17 | 3 |
| LW 129 | – | < 5 | 3 | 3.7 ± 0.62 | > 95 | 5 | – | – | – |
| LW 131 | – | < 5 | 2 | 4.1 ± 1.6 | > 95 | 2 | – | – | – |
| LW 145 | 3.2 ± 1.2 | − 14 ± 5 | 6/11 | 3.8 ± 0.64 | 88 ± 6 | 5 | – | – | – |
| LW 148 | – | < 5 | 6 | 4.4 ± 1.6 | > 95 | 6 | – | – | – |
| LW 209 | 0.48 ± 0.1 | − 19 ± 3 | 4 | 4.1 ± 1.3 | 96 ± 4 | 3 | – | – | – |
| LWYW22 | – | < 5 | 1 | 3.8 ± 1.5 | > 95 | 2 | – | – | – |
| LF1 | – | − 8 | 2 | 6.8 ± 3.2 | 75 ± 7 | 5 | 11 ± 6.1 | > 95 | 3 |
| LF14 | – | − 15 ± 22 | 2 | 22 ± 16 | 76 ± 17 | 3 | 14.3 ± 5.8 | 53 ± 10 | 3 |
| LF22 | – | − 29 ± 5.6 | 2 | 7.2 ± 3.7 | 63 ± 13 | 3 | 4.3 ± 2.6 | 59 ± 16 | 3 |
aMeasurement of G-protein signaling was performed applying the IP-One assay® (Cisbio) in HEK293T cells transiently co-transfected with the human TAS2R14 receptor and the hybrid G-protein Gαqi
bInhibition of the agonist effect of 1 µM of FFA/aristolochic acid
cPotency of TAS2R14 activation as mean value in µM ± SEM
dMaximum efficacy in % ± SEM relative to the full effect of FFA
eNumber of individual experiments all performed in duplicates/triplicates
fPotency to inhibit the effect of 1 µM FFA as mean value in µM ± SEM
gMaximum inhibitory efficacy was analyzed by subtracting the effect at the highest concentrations of test compound suitable for inhibition from 100% and is displayed as % ± SEM
hPotency to inhibit the effect of 1 µM aristolochic acid as mean value in µM ± SEM