Effect of LY487379 on agonist-evoked [35S]GTPγS stimulation at human mGlu2 receptors
Potency (EC50), and efficacy (Emax) for the stimulation of [35S]GTPγS binding to recombinant human mGlu2 receptors preparation in the absence or presence (+ LY) of 3 μM LY487379. Summary data represent the geometric mean EC50 values (lower-upper S.D.), and mean efficacy ± S.E.M. (compared with glutamate alone), calculated from three individual experiments performed in triplicate. Ratio values are calculated from the EC50 or Emax values obtained by the agonist alone, divided by those obtained in the presence of LY487379.
| Agonists | EC50 | EC50(+ LY) | Ratio (EC50) | Emax | Emax(+ LY) | Ratio(Emax) |
|---|---|---|---|---|---|---|
| nM | nM | |||||
| Glutamate | 8,000(7,000−9,000) | 3,300(2,000−6,000) | 2.4 | 101 ± 2 | 108 ± 5 | 1.1 |
| DCG-IV | 400(270−630) | 270(200−360) | 1.5 | 56 ± 5* | 127 ± 8 | 2.3 |
| LCCG-I | 1,600(600−4,000) | 300(260−400) | 5.3 | 68 ± 10* | 136 ± 7 | 2.0 |
| LY379268 | 17(18−40) | 4(2−9) | 4 | 103 ± 4 | 130 ± 7 | 1.26 |
↵* Significantly different from glutamate (p < 0.01 paired t test).