Table 1.
Structures and Activities of Analogs 10.
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| ||||
Cmpd | NR1R2 | plC50a ±SEM |
IC50 (μM)a | %Glu Minb ±SEM |
7 |
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5.42±0.04 | 3.8 | 10.4±2.1 |
10a |
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5.30±0.06 | 5.0 | 4.4±0.7 |
10b |
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5.61±0.07 | 2.5 | −1.1±0.5 |
10c |
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5.24±0.01 | 5.7 | 2.2±1.1 |
10d |
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>10 | 16.4±2.5 | |
10e |
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5.69±0.04 | 2.1 | 0.5±0.4 |
10f |
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>10 | 7.6±3.2 | |
10g |
![]() |
>10 | 9.6±2.1 |
Measured in an mGlu3 GIRK assay.
% Glu Min is the % inhibition of the compound on an EC80 concentration of glutamate. Values represent the mean ± standard error mean for three independent experiments performed in triplicate.