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. 2016 Apr;89(4):457–466. doi: 10.1124/mol.115.101808

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.

a

P < 0.001, significantly statistically different compared with D2LR (one-way analysis of variance, followed by post hoc Newman-Keuls test).