Afobazole (hydrochloride)

Afobazole is a multi-targeted anxiolytic drug with neuroprotective activities.^1,2 It binds to the sigma-1, melatonin MT₁, and MT₃ receptors, as well as monoamine oxidase A (MAO-A; K_is = 5.9, 160, 0.97, and 3.6 µM, respectively, in a radioligand binding assay).¹ Afobazole (5 mg/kg) decreases the latency to enter, as well as increases the number of entries into and percentage of time spent in, the open arms of the elevated plus maze, indicating anxiolytic-like activity in passive stress-coping BALB/c, but not active stress-coping C57BL/6, mice.³ It decreases stroke volume and neuronal and oligodendroglial cell death in the brain in a rat model of ischemia induced by middle cerebral artery occlusion (MCAO) when administered at doses of 0.3 and 3 mg/kg.²

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1. Seredenin, S.B., and Voronin, M.V. [Neuroreceptor mechanisms of the afobazole effect]. Eksp. Klin. Farmakol. 72(1), 3-11 (2009).

2. Katnik, C., Garcia, A., Behensky, A.A., et al. Treatment with afobazole at delayed time points following ischemic stroke improves long-term functional and histological outcomes. Neurobiol. Dis. 62, 354-364 (2014).

3. Anderzhanova, E.A., Bächli, H., Buneeva, O.A., et al. Strain differences in profiles of dopaminergic neurotransmission in the prefrontal cortex of the BALB/C vs. C57Bl/6 mice: Consequences of stress and afobazole. Eur. J. Pharmacol. 708(1-3), 95-104 (2013).