Table 1.
Agonist and antagonist potency at hFFA2 and rFFA2
| hFFA2 | rFFA2 | ||||
|---|---|---|---|---|---|
| [35S]-GTPγS pEC501 | [35S]-GTPγS pEC50 | LANCE-cAMP (pEC50 and %Effect) | Yeast pXC50 (5 mmol/L 3AT) | rFFA2 Yeast pEC50 | |
| C3 (propionate) | ND2 | 4.5 ± 0.08 n = 2 | 5.2 ± 0.05 (100%) n = 2 | 3.4 ± 0.11 (100%) n = 2 | 3.7 ± 0.20 (100%) n = 2 |
| 4-CMTB | ND2 | 6.9 ± 0.12 n = 3 | 7.1 ± 0.22 118 ± 4% n = 20 | 6.4 ± 0.25 105 ± 14% n = 45 | 7.1 ± 0.11 112 ± 16% n = 22 |
| Compound 14 | 7.0 | 8.2 ± 0.23 n = 4 | 7.7 ± 0.54 109 ± 7% n = 4 | 5.1 ± 0.163 65 ± 5%3 n = 4 | 5.0 ± 0.13 105 ± 18% n = 6 |
| Compound 9 | 7.2 | 7.0 ± 0.08 n = 2 | ∼4 n = 4 | 6.74 ± 0.154 n = 3 | Antagonist |
| Compound 101 | 7.2 | 7.1 ± 0.29 n = 3 | 5.4 ± 0.46 65 ± 10% n = 6 | 6.73 ± 0.234 n = 3 | Antagonist |
| Compound 105 | 7.1 | 8.1 ± 0.48 n = 4 | 7.1 ± 0.47 102 ± 3% n = 5 | 6.45 ± 0.204 n = 3 | Antagonist |
EC50 values for [35S]-GTPγS accumulation (Column 1) were taken from Hoyveda et al. (2010) and converted to pEC50 (-log10[EC50]) for comparison to pEC50 values generated herein (Column 2). Yeast pXC50 values indicate pEC50 values for compounds acting as agonists (C3, 4-CMTB and 14) and pIC50 values for compounds acting as inverse agonists (9, 101 and 105; underlined) in the yeast assay under the condition of 5 mmol/L 3AT. Compounds 9, 101, and 105 antagonized rFFA2 but accurate pIC50 values were not determined. 4-CMTB, 4-chloro-α-(1-methylethyl)-N-2-thiazolyl-benzeneacetamide
1
(Hoyveda et al. 2010)
2
ND: not disclosed
3
estimated (curve upper asymptote was not accurately defined)
4
pIC50 values.