Table 1. Initial Picolinamide Core Analogs of 9.
no. | mGlu5 pIC50 (±SEM)a | mGlu5 IC50 (nM)a | % Glu maxa,b |
---|---|---|---|
9 | 7.62 ± 0.03 | 24 | 1.2 ± 0.1 |
10 | 6.70 ± 0.15 | 200 | 1.2 ± 0.1 |
11 | 7.01 ± 0.09 | 98 | 1.3 ± 0.1 |
12 | 7.22 ± 0.23 | 60 | 1.4 ± 0.1 |
13 | 8.01 ± 0.16 | 10 | 1.3 ± 0.1 |
Calcium mobilization mGlu5 assay; values are an average of n ≥ 3 independent experiments.
Amplitude of response in the presence of 30 μM test compound as a percentage of maximal response (100 μM glutamate); an average of n ≥ 3 independent experiments.