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编 号:F459117
分子式:C13H11N3O
分子量:225.25
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10mM*1mL in DMSO
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2mg
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5mg
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10mg
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25mg
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生物活性:
FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of?β-adrenoceptors in mouse cerebral cortex.

体内研究:
FG-7142 (intraperitoneal?injection; 15-30 mg/kg) activates mesolimbocortical dopaminergic projections, leading to increases in dopamine in the prefrontal cortexandthe 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.

体外研究:
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 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 (EC50: α2= 507 nM,α3=1.021μM , α5=1.439 μM).
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