DAA1106

TSPO激动剂（在放射性配体结合试验中IC50=0.28nM）；浓度大于10µM时，对大鼠全脑膜中的TSPO具有选择性，而对CBR和GABAA受体以及54个离子通道、摄取/转运蛋白和次级信使受体均有选择性；增加大鼠脑匀浆中线粒体孕烯醇酮的形成，从而间接增强GABAA受体信号传导；以剂量依赖性方式增加小鼠在明暗探索的明亮区域内停留的时间以及大鼠在高架十字迷宫的开放臂内停留的时间，表明焦虑样行为减少；已合成放射性标记版本，以使用PET研究神经系统疾病模型中PBR的分布。A TSPO agonist (IC50 = 0.28 nM in a radioligand binding assay); selective for TSPO over CBR and GABAA receptors in rat whole brain membranes, as well as a panel of 54 ion channels, uptake/transporters, and secondary messenger receptors at concentrations greater than 10 µM; increases mitochondrial prognenolone formation in rat brain homogenates, which indirectly potentiates GABAA receptor signaling; increases the time mice spend in the light area of the light/dark exploration and the time rats spend in open arms of the elevated plus maze in a dose-dependent manner, suggesting a decrease in anxiety-like behavior; radiolabeled versions have been synthesized to study the distribution of PBRs in neurological disease models using PET.