Functional activity of JNJ-40068782, BINA, LY487379, and LY2607540 at human and rat recombinant mGlu2 receptors, in the absence or presence of an EC20 concentration of glutamate
Values are an average of 6–13 experiments. Emax values are indicated as mean ± S.E.M.; EC50 values are geometric means with 95% CIs indicated in parentheses.
| Compound | Activity in Absence of Glutamate | Activity in Presence of EC20 Glutamate | ||
|---|---|---|---|---|
| Emax | EC50 | Emax | EC50 | |
| % | nM | % | nM | |
| Human mGlu2 | ||||
| JNJ-40068782 | 69 ± 9 | 925 (573–1493) | 309 ± 23 | 143 (108–190) |
| BINA | 60 ± 3 | 572 (141–2324) | 221 ± 9 | 89 (48–162) |
| LY487379 | 20 ± 3 | >50.000 | 147 ± 9 | 256 (193–337) |
| LY2607540 | 28 ± 2 | 720 (631–821) | 215 ± 7 | 95 (77–117) |
| Rat mGlu2 | ||||
| JNJ-40068782 | 31 ± 3.7 | >30.000 | 444 ± 86 | 307 (287–327) |
| BINA | 35 ± 4.9 | >30.000 | 390 ± 63 | 138 (57–336) |
| LY487379 | 7.4 ± 3.9 | >30.000 | 166 ± 14 | 501 (417–602) |
| LY2607540 | 13 ± 1.5 | >30.000 | 273 ± 10 | 314 (251–392) |