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首页-小分子抑制剂&激动剂-GPCR-5-HT Receptor-Prucalopride
Prucalopride

Chemical Structure : Prucalopride

CAS No.: 179474-81-8

Prucalopride (R-108512, R108512)

货号: PC-23280Not For Human Use, Lab Use Only.

Prucalopride (R-108512) is a potent, selective 5-HT4 receptor agonist with pKi of 8.6 and 8.1 for 5-HT4a and 5-HT4b, >290-fold higher affinity for 5-HT4 receptors than for other receptors.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Prucalopride (R-108512) is a potent, selective 5-HT4 receptor agonist with pKi of 8.6 and 8.1 for 5-HT4a and 5-HT4b, >290-fold higher affinity for 5-HT4 receptors than for other receptors.
Prucalopride targets the impaired motility associated with chronic constipation, thus normalizing bowel movements.
Prucalopride induces contractions (pEC50=7.48) in the guinea-pig colon, demonstrates anti-cholinergic, anticholinesterase or nonspecific inhibitory activity and does not antagonise 5-HT2A, 5-HT2B and 5-HT3 receptors or motilin, CCK1 receptors.

物理化学性质&存储条件

分子量 367.87
分子式 C18H26ClN3O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

参考文献

1. Prins NH, et al. Br J Pharmacol. 1999 Jul;127(6):1431-7.

2. Poen AC, et al. Aliment Pharmacol Ther. 1999 Nov;13(11):1493-7.

3. Briejer MR, et al. Eur J Pharmacol. 2001 Jun 29;423(1):71-83.

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