AC-5216 is a high affinity agonist of the 18 kDa translocator protein (TSPO, previously called the peripheral benzodiazepine receptor) that exhibits a Ki value of 0.297 nM in rat whole brain and IC50 values of 2.73 and 3.04 nM, respectively, against human and rat glial TSPO.1 AC-5216 produces anxiolytic and antidepressant effects in various animal models, without inducing benzodiazepine-like adverse effects.1,2
1.Kita, A., Kohayakawa, H., Kinoshita, T., et al.Antianxiety and antidepressant-like effects of AC-5216, a novel mitochondrial benzodiazepine receptor ligandBr. J. Pharmacol.1421059-1072(2004) 2.Qiu, Z.K., Zhang, L.M., Zhao, N., et al.Repeated administration of AC-5216, a ligand for the 18 kDa translocator protein, improves behavioral deficits in a mouse model of post-traumatic stress disorderProg. Neuropsychopharmacol. Biol. Psychiatry4540-46(2013)