产品描述:
DAA1106 is an agonist of the 18 kDa translocator protein TSPO, which was previously known as the peripheral benzodiazepine receptor (PBR), that has an IC50 value of 0.28 nM in a radioligand binding assay.{41208} It is selective for TSPO over central benzodiazepine receptors (CBRs) 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. DAA1106 increases mitochondrial prognenolone formation in rat brain homogenates, which indirectly potentiates GABAA receptor signaling. DAA1106 (1-10 mg/kg) 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. Various radiolabeled versions of DAA1106 have been synthesized to study the distribution of PBRs in neurological disease models using positron emission tomography (PET).{41209,41210}