TABLE 4

β arrestin-2 recruitment induced by dopamine and norepinephrine mediated by D2LR, D2SR, D3R, D4.2R, D4.4R, and D4.7R

Results were obtained from β arrestin-2 recruitment-BRET experiments in HEK-293T cells transiently transfected with different D2-like receptors fused to RLuc8 and β arrestin-2 fused to mVenus. Data of individual experiments were fit by nonlinear regression to a sigmoidal dose–response relationship against the agonist concentration. The EC50 and Emax values are the mean ± S.E.M. of 5 to 15 experiments performed in triplicate. Emax values are expressed as 1000 × [BRETmax − BRETbasal].

ReceptorDopamineNorepinephrineNE/DA (EC50)
EC50 (nM)EmaxEC50 (nM)Emax
D2LR96 ± 1611 ± 14800 ± 172011 ± 250
D2SR105 ± 2118 ± 2a2880 ± 115017 ± 227.4
D3R3 ± 1b15 ± 2c32 ± 5c13 ± 210.7
D4.2R38 ± 13c9 ± 13750 ± 162010 ± 2100
D4.4R66 ± 138 ± 12830 ± 6667 ± 143
D4.7R44 ± 12c9 ± 11840 ± 8898 ± 241.8
  • NE/DA, ratio between EC50 values of norepinephrine and dopamine for each receptor.

  • a P < 0.01, compared with D2LR (one-way analysis of variance, followed by post hoc Newman-Keuls test).

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

  • c P < 0.05, compared with D2LR (one-way analysis of variance, followed by post hoc Newman-Keuls test).