TABLE 2

Activation of hD3, hD2L, and hD2S receptors by S32504 and ropinirole as determined by measures of total G-protein activation ([35S]GTPγS binding), Gαi3 activation (immunoprecipitation coupled to SPA detection), and MAP kinase phosphorylation (immunoblot) Data are means ± S.E.M. of ≥3 determinations, each performed in triplicate.



hD3

hD2L

hD2S Total G-Protein
Total G-Protein
i3
MAP Kinase
Total G-Protein
i3
MAP Kinase

pEC50
% Emax
pEC50
% Emax
pEC50
% Emax
pEC50
% Emax
pEC50
% Emax
pEC50
% Emax
pEC50
% Emax
S32504 8.66 ± 0.20 74 ± 3 8.64 ± 0.07 68 ± 2 8.45 ± 0.15 85 ± 5 6.71 ± 0.02 50 ± 3 6.63 ± 0.09 51 ± 1 8.59 ± 0.15 100 ± 6 6.39 ± 0.07 87 ± 1
Ropinirole
7.56 ± 0.09a
59 ± 4a
8.09 ± 0.04
60 ± 3
8.51 ± 0.11
80 ± 8
6.38 ± 0.09a
52 ± 3a
6.48 ± 0.06
55 ± 5
8.21 ± 0.07
98 ± 2
6.18 ± 0.10a
108 ± 2a
  • pEC50, -log (effective concentration50); h, human.

  • a From Millan et al. (2002)