VU0364572 and VU0357017 induce Ca responses in hM1 TREx CHO cells treated across a range of TET concentrations
| TET concentration | CCh | VU0364572 | VU0357017 | |||
|---|---|---|---|---|---|---|
| EC 50 (in μm) | % CCh max | EC 50 (in μm) | % CCh max | EC 50 (in μm) | % CCh max | |
| 0 ng/ml (n =3) | 2.46 (0.72) | 100 (3.45) | 30.5 (12.5) | 44.2 (9.58) | NA | 8.24 (5.06) |
| 10 ng/ml (n =3) | 2.94 (0.82) | 100 (12.8) | 146 (120) | 39.9 (13.5) | 16 (11) | 7.21 (6.24) |
| 25 ng/ml (n =3) | 1.99 (0.69) | 100 (6.40) | 2.3 (1.7) | 68.1 (13.6) | 16 (14) | 24.5 (5.53) |
| 50 ng/ml (n =3) | 1.08 (0.84) | 100 (2.93) | 1.0 (0.4) | 78.1 (5.95) | 1.6 (0.57) | 60.4 (11.1) |
| 1 μg/ml (n =3) | 0.06 (0.01) | 100 (1.29) | 0.5 (0.1) | 86.2 (3.75) | 0.69 (0.24) | 75.3 (1.07) |
CCh induces a near maximum response in untreated cells. A decrease in the potency values was present in cells treated with 50 or 1 μg of TET suggesting the presence of receptor reserves. In cells treated 25, 50, or 1 μg TET, VU0364572 and VU0357017 induces an increase in Emax values. Both compounds were found to be more potent following treatment of cells across a range of TET concentrations. Values in parentheses are SEM.