Molecular Formula | C13H11N3O
|
Molar Mass | 225.25 |
Density | 1.328±0.06 g/cm3(Predicted) |
Boling Point | 576.3±30.0 °C(Predicted) |
Solubility | ethanol: 1mg/mL |
Color | light tan |
pKa | 13.44±0.46(Predicted) |
Storage Condition | 2-8°C |
Use | FG 7142 (ZK 39106; LSU-65) is a non-selective benzodiazepine inverse agonist with high affinity (Ki = 91 nM) for GABAA receptor containing α1 subunit. FG 7142 (ZK 39106; LSU-65) also regulates GABA-induced chlorine flux (EC50=137 nM) on GABAA receptors expressing the α1 subunit. FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and lead to upregulation of β-adrenoceptors in mouse cerebral cortex. |
In vitro study | 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). |
In vivo study | FG-7142 (intraperitonealinjection; 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 (intraperitonealinjection; 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. |