FG 7142 (LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 can increase tyrosine hydroxylation and cause upregulation of β-adrenoceptors in mouse cerebral cortex. FG 7142 , a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM).

GABAA receptor:ki： 91 nM

FG-7142 has a high efficacy in modulating GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50 = 137 nM) as compared to the other α subunits.FG-7142 has affinity for those expressing the α subunit, the Ki values are 91 nM; 330 nM; 492 nM and 2.150 μM for α1, α2,α3 and α5 subunits, respectively.

FG-7142, administered via intraperitoneal injection at doses of 15 mg/kg, enhances tyrosine hydroxylase activity and dopamine turnover specifically in the medial prefrontal cortex and ventral tegmentum, without impacting mesolimbic or nigrostriatal regions. At doses between 15-30 mg/kg, it stimulates mesolimbocortical dopaminergic projections, resulting in elevated dopamine levels in the prefrontal cortex and nucleus accumbens in rats.