靶点：GABA Receptor 通路：Neuronal Signaling;GPCR & G Protein 背景说明：Baclofen是一种有效,选择性的代谢型 GABA-B 受体 (GABABR) 激动剂。 生物活性：Baclofen是GABA衍生物，被用作骨骼肌的弛缓药和中枢神经系统抑制剂。它能够激活GABA receptors，尤其是GABAB受体。[2] In Vitro：Baclofen induces G0/G1 phase arrest which is connected with down-regulation of intracellular cAMP level，and up-regulation of p21WAF1 protein expression as well as its phosphorylation level in human hepatocellular carcinoma cell[3]. In Vivo：Chronic treatment with baclofen markedly diminishes hippocampal atrophy and neuronal apoptosis in hippocampal CA1 area via the regulation of autophagy in chronic cerebral hypoperfusion in rats. Baclofen might suppress cytodestructive autophagic activity through Akt-GSK-3β-p-mTOR-Beclin 1 signaling pathway under chronic cerebral hypoperfusion. During brain ischemia，baclofen could reduce CX43 and CX36 surface expression. Baclofen-induced suppression of increased CX43 and CX36 surface expressions helps neurons survive[1]. Baclofen reduces reinstatement to cocaine self-administration in an animal model of relapse[2]. Baclofen suppresses Bel-7402 xenograft tumor growth in vivo[3]. 细胞实验：Animal Models: male Sprague-Dawley rats of clean grade，aged 2-3 months，weighing 220-250 g; Dosages: 12.5 mg/kg and 25 mg/kg; Administration: i.p.[1] 动物实验：Bel-7402，HuH-7，and HepG2 cells are seeded into 96-well plates(10，000 per well)in a final volume of 200 μl medium. After a 24-hour attachment，cells are incubated with Bac(25，50 and 100 μM)in the absence or presence of Pha(100 μM)for indicated time intervals. During this time，the culture medium is replaced with fresh medium every 24 h. After treatment，cell proliferation is evaluated by MTS assay. The OD values are measured at 490 nm with a microplate spectrophotometer.[3] 数据来源文献：[1] Li Liu， et al. Scientific Reports. 2015， 5: 14474. [2] Di Ciano P， et al. Neuropsychopharmacology. 2003， 28(3):510-8. [3] Wang T， et al. Life Sci. 2008， 82(9-10):536-41.
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