Prucalopride (succinate) | 琥珀酸普芦卡必利

MCE 国际站：Prucalopride (succinate)

中文名：琥珀酸普芦卡必利

CAS：179474-85-2

品牌：MedChemExpress (MCE)

存储条件：4°C, sealed storage, away from moisture

生物活性：Prucalopride succinate 是一种选择性、高亲和力的 5-HT4 受体激动剂，对 5-HT4a/4b 的 pKi 为 8.6/8.1。 IC50 值：目标：体外 5-HT4 激动剂：普卢卡必利是豚鼠结肠中的 5-HT(4) 受体激动剂，因为它诱导收缩（pEC(50)=7.48+/-0.06；对 5 不敏感-HT(2A) 或 5-HT(3) 受体拮抗剂，但被 5-HT(4) 受体拮抗剂抑制）以及促进电刺激诱导的非胆碱能收缩（被 5-HT(4) 阻断）受体拮抗剂）。普卢卡必利不会引起 5-HT(2A)、5-HT(2B) 或 5-HT(3)、促胃动素或胆囊收缩素 (CCK(1)) 受体介导的收缩的相关抑制，也不会抑制烟碱或毒蕈碱乙酰胆碱受体-介导的收缩，高达 10 microM [1]。体内：大鼠微透析研究表明，普卢卡必利在 5 和 10 mg/kg 时最大程度地增加了前额皮质中的 ACh 和组胺水平，而 PRX-03140 在 50 mg/kg 时显着增加了皮质组胺水平，但在较低剂量下未能影响 ACh 释放超过 150 毫克/千克 [2]。

体外：Prucalopride succinate (10 µM; 24, 48, 72 h) 在A549细胞中显示抗增殖活性[4]。 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[4]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内：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[2]。 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[3]。 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[3]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Diabetes mellitus (DM) rat models[3] 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). Clinical Trial

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研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Apoptosis  |  Autophagy

作用靶点：5-HT Receptor  |  Apoptosis  |  Autophagy

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参考文献：[1]. 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.

[2]. Johnson DE, et al. The 5-hydroxytryptamine4 receptor agonists prucalopride and PRX-03140 increase acetylcholine and histamine levels in the rat prefrontal cortex and the power of stimulated hippocampal θ oscillations. J Pharmacol Exp Ther. 2012 Jun;341(3):681-91

[3]. 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.

[4]. 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.