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编 号:F215997
分子式:C22H32ClN3O7
分子量:485.96
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10mM*1mL in DMSO
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5mg
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10mg
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50mg
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100mg
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200mg
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生物活性:
Prucalopride succinate is an orally active, selective and specific 5-HT 4 receptor agonist (high affinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride succinate improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride succinate also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride succinate can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer.

体内研究:
Prucalopride succinate (5 mg/kg, 皮下注射) 可增加大鼠前额皮质乙酰胆碱和组胺水平。Prucalopride succinate (5, 10 μg/kg;口服;每天一次连续两周) 可缩短DM模型结肠转运时间,促进结肠神经干细胞和神经元再生。Prucalopride succinate (5, 10 μg/kg;口服;每天一次连续两周)可促进结肠神经干细胞分化,激活胶质蛋白表达,一定程度上促进神经元损伤的恢复。Animal Model:Diabetes mellitus (DM) rat models
Dosage:5 μg/kg, 10 μg/kg
Administration:Oral gavage, single daily for 2 weeks.
Result:Accelerated colonic movement and shortened the colonic transit time, and markedly increased the expression levels of Ki67 .Increased expression of SOX10 in the columnar epithelial nuclei and enteraden (when at 5 μg/kg), and in the columnar epithelial cells, the nuclei of lamina propria cells and enteraden (when at 10 μg/kg). Significantly increased Nestin expression, which concentrated in columnar epithelial cells and the mesenchyme. (Nestin:a marker of enteric neural stem cells in the ENS).

体外研究:
Prucalopride succinate (10 μM; 24, 48, 72 h) 在A549细胞中显示抗增殖活性。Prucalopride succinate 诱导A549/A427细胞自噬和凋亡,降低磷酸化蛋白激酶B (AKT)和哺乳动物雷帕霉素靶蛋白(mTor)的表达。
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