DAA1106

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.¹ It is selective for TSPO over central benzodiazepine receptors (CBRs) and GABA_A 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 GABA_A 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).^2,3

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1. Okuyama, S., Chaki, S., Yoshikawa, R., et al. Neuropharmacological profile of peripheral benzodiazepine receptor agonists, DAA1097 and DAA1106. Life Sci. 64(16), 1455-1464 (1999).

2. Zhang, M.-R., Kida, T., Noguchi, J., et al. [¹¹C]DAA1106: radiosynthesis and in vivo binding to peripheral benzodiazepine receptors in mouse brain. Nucl. Med. Biol. 30(5), 513-519 (2003).

3. Venneti, S., Wagner, A.K., Wang, G., et al. The high affinity peripheral benzodiazepine receptor ligand DAA1106 binds specifically to microglia in a rat model of traumatic brain injury: Implications for PET imaging. Exp. Neurol. 207(1), 118-127 (2007).