产品
编 号:F215996
分子式:C18H26ClN3O3
分子量:367.87
产品类型
结构图
CAS No: 179474-81-8
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产品详情
生物活性:
Prucalopride 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 improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer.
体内研究:
Prucalopride (5, 10 μg/kg; p.o.; single daily for 2 weeks) shortens the colonic transit time in DM model, promotes the regeneration of colonic neural stem cells and neurons.Prucalopride (5, 10 μg/kg; p.o.; single daily for 2 weeks) promotes the differentiation of colonic neural stem cells, activates the expression of glial proteins and promotes the recovery of neuronal injury to a certain extent.Animal Model:Sprague dawley rats (diabetes mellitus (DM) model).
Dosage:5 or 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 (10 μM; 24, 48, 72 h) shows anti proliferative activity in A549 cells.Prucalopride induces autophagy and apoptosis, decreases the expression of the phosphorylated protein kinase B (AKT) and mammalian target of rapamycin (mTor) in A549/A427 cells.