| Bioactivity | 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[1][2][3]. | ||||||||||||
| Invitro | Prucalopride (10 µM; 24, 48, 72 h) shows anti proliferative activity in A549 cells[1].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[1]. Cell Proliferation Assay[1] Cell Line: | ||||||||||||
| 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[2].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[2]. Animal Model: | ||||||||||||
| Name | Prucalopride | ||||||||||||
| CAS | 179474-81-8 | ||||||||||||
| Formula | C18H26ClN3O3 | ||||||||||||
| Molar Mass | 367.87 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Chen M, et al. Prucalopride inhibits lung cancer cell proliferation, invasion, and migration through blocking of the PI3K/AKT/mTor signaling pathway. Hum Exp Toxicol. 2020 Feb;39(2):173-181. [2]. Wang Y, et al. Prucalopride might improve intestinal motility by promoting the regeneration of the enteric nervous system in diabetic rats. Int J Mol Med. 2022 Jul;50(1):87. [3]. Briejer MR, et al. The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound. Eur J Pharmacol. 2001 Jun 29;423(1):71-83. |