TABLE 1

Activity of LY487379 on glutamate-induced [35S]GTPγS binding.

Concentration-response curves were determined in the presence of 1 μM glutamate in membranes prepared from rat brain or recombinant cells expressing hmGlu2 receptors, or 10 nM glutamate for the hmGlu3 receptor preparation. 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.

Membrane Preparation EC50Emax
μM
Rat brain (cortex) 2.8 (2.1−3.7) 68 ± 4
hmGluR2 1.7 (0.7−4.0) 52 ± 4
hmGluR3 N.E. N.E.
  • N.E., no effect at concentrations up to 10 μM.