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

DAA1106 – 500 µg

Brand:
Cayman
CAS:
220551-92-8
Storage:
-20
UN-No:
Non-Hazardous - /

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}  

 

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Description

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

Formal name: N-[(2,5-dimethoxyphenyl)methyl]-N-(5-fluoro-2-phenoxyphenyl)-acetamide

Synonyms: 

Molecular weight: 395.4

CAS: 220551-92-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Activators||Research Area|Neuroscience|Behavioral Neuroscience|Anxiety

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