FG 7142

FG 7142 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) . 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 (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.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.