Table 2. Functional Activity of Representative mGluR2 PAMs 5, 41−68a.
| compound | R2 | mGlu2 EC50 (μM)a | mGlu2 Emax (%) |
|---|---|---|---|
| 5 | Ph- | 6.29 | 138 |
| 41 | 2-F-Ph- | 1.00 | 44 |
| 42 | 3-F-Ph- | 1.91 | 96 |
| 43 | 4-Cl-Ph- | 1.41 | 189 |
| 44 | 4-OH-Ph- | >10 | |
| 45 | 4-CF3O-Ph- | 0.24 | 228 |
| 46 | 2,3-diF-Ph- | 10 | 131 |
| 47 | 2,4-diF-Ph- | 4.79 | 128 |
| 48 | 2,4,6-triF-Ph- | 2.96 | 118 |
| 49 | 3-F-4-Cl-Ph- | 0.48 | 180 |
| 50 | 2-F-4-CF3−Ph- | 3.16 | 124 |
| 51 | 3-Py- | >10 | |
| 52 | 3-(6-MeO)Py- | 6.03 | 66 |
| 53 | 3-(6-CF3)Py- | 6.76 | 144 |
| 54 | 4-(2-Me)-triazolyl- | >10 | |
| 55 | 2-benzimidazolyl- | >10 | |
| 56 | 2-benzothiazolyl- | 5.62 | 79 |
| 57 | PhCH2CH2- | 3.71 | 117 |
| 58 | PhOCH2- | 3.98 | 87 |
| 59 | 3-Cl-PhOCH2- | 3.16 | 124 |
| 60 | 4-Cl-PhOCH2- | 1.91 | 115 |
| 61 | n-propyl- | 7.24 | 53 |
| 62 | n-butyl- | 9.28 | 122 |
| 63 | i-butyl- | 0.54 | 75 |
| 64 | s-butyl- | 12.88 | 97 |
| 65 | CF3CH2CH2- | 8.71 | 97 |
| 66 | cyclopentyl- | 9.33 | 122 |
| 67 | cyclohexyl- | 0.43 | 120 |
| 68 | cyclohexylmethyl- | 1.08 | 161 |
Values are means of three experiments.
