Table 3

Potencies of various mGlu1 receptor agonists and antagonists in inhibition of [3H]quisqualate binding to rat mGlu1a receptor CHO-dhfr- membranes.

CompoundKiHill Coefficient
μM
Quisqualate0.030  ± 0.000.98  ± 0.01
Glutamate0.40  ± 0.070.99  ± 0.01
LY3673851.18  ± 0.470.99  ± 0.01
(S)-3,5-DHPG1.42  ± 0.000.97  ± 0.00
(S)-4C3HPG1.65  ± 0.060.98  ± 0.02
(1S,3R)-ACPD1.92  ± 0.200.97  ± 0.01
(S)-4CPG4.51  ± 0.780.98  ± 0.00
AIDA98.3  ± 15.40.98  ± 0.03
MCPG165  ± 0.470.96  ± 0.02
R214127>1,000
NPS 2390>1,000
BAY 36–7620>1,000
CPCCOEt>1,000

Ki values and Hill coefficients are mean ± S.D. of two independent experiments.