TABLE 3

Summary of antagonist properties of S33138 at hD3, hD2L, and hD2S receptors as determined by blockade of DA-stimulated [35S]GTPγS binding, Gαi3 recruitment, and extracellular-regulated-kinase (ERK) phosphorylation

Data (pKi and pKB values) are means ± S.E.M. of three to four independent experiments.


hD3
[3H]Spiperone
[35S]GTPγS
SPA (Gαi3)
ERK1/2
pKi
pKB
% MOI
pKB
% MOI
pKB
% MOI



8.68 ± 0.01
8.85 ± 0.10
97 ± 3
8.24 ± 0.07
95 ± 7
9.08 ± 0.02
104 ± 4



hD2L
hD2S
[3H]Spiperone
[35S]GTPγS
SPA (Gαi3)
ERK1/2
[3H]Spiperone
[35S]GTPγS
pKi
pKB
% MOI
pKB
% MOI
pKB
% MOI
pKi
pKB
% MOI
7.13 ± 0.03
7.82 ± 0.03
104 ± 8
7.76 ± 0.14
83 ± 12
8.03 ± 0.02
101 ± 2
7.26 ± 0.08
7.79 ± 0.06
96 ± 5
  • MOI, maximal observed inhibition.