TABLE 2.
Adenylyl cyclase inhibition by dopamine and norepinephrine mediated by D2LR, D2SR, D3R, D4.2R, D4.4R, and D4.7R
Results are from adenylyl cyclase inhibition-BRET experiments in HEK-293T cells transiently transfected with the CAMYEL sensor and one of the indicated receptors. Data were fit by nonlinear regression to a sigmoidal dose–response relationship against the agonist concentration. The EC50 and Emax values are mean ± S.E.M. of 5 to 11 experiments performed in triplicate. Emax values are expressed as 1000 × [BRETmax − BRETbasal].
Receptor | Dopamine |
Norepinephrine |
NE/DA (EC50) | ||
---|---|---|---|---|---|
EC50 (nM) | Emax | EC50 (nM) | Emax | ||
D2LR | 9.4 ± 1.1 | 94 ± 8 | 88 ± 17 | 94 ± 6 | 9.4 |
D2SR | 6.7 ± 0.5a | 140 ± 7a | 62 ± 6 | 149 ± 8a | 9.3 |
D3R | 1.6 ± 0.2a | 48 ± 7a | 19 ± 3a | 50 ± 5a | 12 |
D4.2R | 1.8 ± 0.2a | 74 ± 8 | 54 ± 8 | 69 ± 8 | 30 |
D4.4R | 1.4 ± 0.2a | 98 ± 9 | 53 ± 8 | 79 ± 6 | 38 |
D4.7R | 1.6 ± 0.3a | 83 ± 11 | 53 ± 13 | 84 ± 6 | 33 |
NE/DA, ratio between EC50 values of norepinephrine and dopamine for each receptor.
P < 0.001, significantly statistically different compared with D2LR (one-way analysis of variance, followed by post hoc Newman-Keuls test).