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CAS No. : 78538-74-6
MCE 国际站:FG 7142
产品活性:FG 7142 (ZK 39106; LSU-65) 是一种非选择性的苯二氮杂卓反向激动剂,对含 α1 亚基的 GABAA receptor 具有高亲和力 (Ki= 91 nM)。FG 7142 (ZK 39106; LSU-65) 还调节表达 α1 亚基的 GABAA 受体上 GABA 诱导的氯通量 (EC50= 137 nM)。FG 7142 (ZK 39106; LSU-65) 可以增加酪氨酸羟化并导致小鼠大脑皮层中 β-肾上腺素受体的上调。
研究领域:Membrane Transporter/Ion Channel | Neuronal Signaling
作用靶点:GABA Receptor
In Vitro: 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).
In Vivo: 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.
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