Table 1.
Functional characterization of agonists C1-C12 as determined by cAMP production in whole cells
| Compound | EC50 (μM) | Rmin (% FSK) | Rmax (% FSK) | R2 | Hill coefficient |
| C1-S | 4.23 ± 1.00 | 9.44 ± 0.88 | 66.98 ± 2.84 | 0.958 ± 0.005 | 1.068 ± 0.159 |
| C2-S | 6.67 ± 2.01 | 11.76 ± 2.6 | 66.47 ± 0.86 | 0.952 ± 0.012 | 1.210 ± 0.041 |
| C3-S | 4.31 ± 1.69 | 8.40 ± 1.40 | 62.24 ± 6.59 | 0.949 ± 0.018 | 1.131 ± 0.076 |
| C4-S | 3.52 ± 0.52 | 10.29 ± 4.77 | 43.53 ± 11.67 | 0.914 ± 0.024 | 2.827 ± 0.291 |
| C5-S | 7.66 ± 0.95 | 8.16 ± 0.64 | 68.76 ± 10.30 | 0.970 ± 0.007 | 0.948 ± 0.026 |
| C6-S | 6.53 ± 0.89 | 8.83 ± 0.92 | 68.74 ± 6.21 | 0.896 ± 0.058 | 0.819 ± 0.150 |
| C7-S | >100 | 3.18 ± 2.27 | N/A | N/A | N/A |
| C8-S | 8.35 ± 1.50 | 5.75 ± 1.42 | 22.87 ± 5.11 | 0.950 ± 0.010 | 1.724 ± 0.086 |
| C9-S | 6.87 ± 0.81 | 10.37 ± 1.29 | 47.79 ± 5.28 | 0.946 ± 0.003 | 1.648 ± 0.103 |
| C10-S | 16.72 ± 3.06 | 11.01 ± 0.63 | 50.32 ± 3.73 | 0.956 ± 0.003 | 1.643 ± 0.052 |
| C11-S | 5.94 ± 0.46 | 12.78 ± 3.39 | 46.44 ± 8.89 | 0.945 ± 0.017 | 2.764 ± 0.379 |
| C12-S | 1.64 ± 0.35 | 14.28 ± 3.03 | 35.89 ± 5.25 | 0.904 ± 0.028 | 3.588 ± 0.462 |
CHW cells were stably transfected to express human β2AR, and cAMP levels determined after a 10-min exposure to multiple concentrations of the indicated agonists. The EC50 for isoproterenol = 2.5 nM, with Rmax-Rmin values = 52.3. FSK, forskolin; N/A, not applicable due to lack of curve fit.