Prucalopride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Prucalopride 是一种选择性、高亲和力 5-HT 受体激动剂，针对 5-HT4A 和 5-HT4B 受体，Ki 分别为 2.5 nM 和 8 nM。

Prucalopride is a selective, high affinity 5-HT receptor agonist for 5-HT4A and 5-HT4B receptor with Ki of 2.5 nM and 8 nM, respectively, exhibits >290-fold selectivity against other 5-HT receptor subtypes.(In Vitro):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.(In Vivo):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.

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. Cell Proliferation Assay Cell Line:A549 cells Concentration:10 μM Incubation Time:24, 48, 72 h Result:Repressed lung cancer cells proliferation.

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).

Prucalopride | Prucalopride free base

Endocrinology/Hormones

5-HT Receptor

5-HT1A| 5-HT1B| 5-HT3| 5-HT4A| 5-HT4B

Neurological Disease

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179474-81-8

367.87

C18H26ClN3O3

>98% (HPLC)

Ethanol: 38 mg/mL (103.29 mM); DMSO: 60 mg/mL (163.1 mM)

ClC1=CC(C(NC2CCN(CCCOC)CC2)=O)=C3C(CCO3)=C1N

4-amino-5-chloro-N-(1-(3-methoxypropyl)piperidin-4-yl)-2,3-dihydrobenzofuran-7-carboxamide

(-20℃)

With Ice Pack

≥ 2 years