Fig. 2From: Design, synthesis, and characterization of novel system xC− transport inhibitors: inhibition of microglial glutamate release and neurotoxicityMicroglial Glu release assay. Rat primary microglia were activated with 100 ng/ml LPS alone or immediately following application of the indicated concentrations of test substances. After 18 h in the presence of LPS, an aliquot of medium was assayed for Glu via a glutamate dehydrogenase colorimetric assay. A First generation of compounds was created by simply varying the position of a methyl group around an aromatic ring, comparing activity to 3,5-DBT. B Additional modifications were evaluated, including several that simply extend the size of the structure hypothesized to fit into the hydrophobic pocket of the SxC− transporter. Values are represented relative to the Glu detected in cultures treated with LPS alone; each data point represents a mean of 4 cultures. Nonlinear regression was performed to provide the plot linesBack to article page