TABLE 4

Activity of MRLSD-064, MRLSD-726, MRLSD-438, and MRLSD-667 on glutamate-induced [35S]GTPγS binding

Concentration-response curves were determined in the presence of 1 μM glutamate in rat brain membranes and mGluR2-containing membranes from stably transfected cells. For the hmGluR3-containing membranes from stably transfected cells, 10 nM glutamate was used. Results are expressed as mean EC50 values (lower-upper S.D.) and mean efficacy (Emax) ± S.E.M., expressed relative to the maximal stimulation achieved by glutamate alone. Summary data are calculated from three individual experiments performed in triplicate.


Compound

hmGluR2

hmGluR3

Rat Brain
Maximum
EC50
Maximum
EC50
Maximum
EC50
μM μM μM
MRLSD-064 115 91 ± 27 136 947 ± 498 124 452 ± 208
MRLSD-726 125 55 ± 43 130 587 ± 572 185 178 ± 30
MRLSD-438 97 46 ± 9 89 845 ± 112 243 545 ± 184
MRLSD-667
114
120 ± 71
120
438 ± 436
129
415 ± 113