Table 2

Functional Parameters of WT, R3, B2, B3, and R3B3 coupling to Gi and Gs

GiCouplingGS Coupling
Max InhibitionEC50Max StimulationEC50
% nM % over control nM
WT850.1516041
R3870.2100240
B2823.018039
B3717.480240
R3B3642820190

[3H]cAMP accumulation assays were performed on whole cells that had been pretreated with (GS coupling) or without (Gi coupling) PTX. Cells were incubated with increasing concentrations of UK 14,304 for 30 minutes at 37° in the presence of 1 mM IBMX and 30 μM forskolin. Maximum responses and EC50values were determined from dose response curves. Data are from three or four separate experiments performed in duplicate.