Table 2. Succinimide SAR.
| entry | R | rat mGlu1 pIC50 (±SEM)a | rat mGlu1 IC50 (nM) | rat % Glu Max (±SEM)ab | human mGlu1 pIC50 (±SEM)a | human mGlu1 IC50 (nM) | human % Glu Max (±SEM)ab |
|---|---|---|---|---|---|---|---|
| 9 | A | 6.60 ± 0.03 | 249 | 1.4 ± 0.2 | <5.0c | >10 000 | 55.1 ± 7.1 |
| 18 | B | <4.5 | >30 000 | <4.5 | >30 000 | ||
| 19 | C | <4.5 | >30 000 | <4.5 | >30 000 | ||
| 20 | D | <4.5 | >30 000 | <4.5 | >30 000 | ||
| 21 | E | <4.5 | >30 000 | <4.5 | >30 000 | ||
| 22 | F | <4.5 | >30 000 | <4.5 | >30 000 |
a
Values are average of n ≥ 3.
b
Amplitude of response in the presence of 30 μM test compound as a percentage of maximal response (100 μM glutamate); average of n ≥ 3.
c
CRC does not plateau.