Ki: 91 nM (GABAA receptor)

FG-7142 has affinity for those expressing the α subunit, the K _i values are 91 nM; 330 nM; 492 nM and 2.150 μM for α1, α2,α3 and α5 subunits, respectively. FG-7142 has a high efficacy in modulating GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC ₅₀ = 137 nM) as compared to the other α subunits (EC ₅₀ : α2= 507 nM,α3=1.021μM , α5=1.439 μM).

FG-7142 (intraperitoneal?injection; 15-30 mg/kg) activates mesolimbocortical dopaminergic projections, leading to increases in dopamine in the prefrontal cortex and the nucleus accumbens in rats. FG-7142 (intraperitoneal?injection; 15 mg/kg) increases tyrosine hydroxylase activity and dopamine turnover in the medial prefrontal cortex and ventral tegmentum in vivo, but effects are not detected in mesolimbic or nigrostriatal areas.