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Prucalopride Succinate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Prucalopride Succinate图片
CAS NO:179474-85-2
包装与价格:
包装价格(元)
50 mg电议
100 mg电议
200 mg电议
500 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
琥珀酸普芦卡必利
R-108512
琥珀酸普卡比利
Resolor Succinate
产品介绍
Prucalopride Succinate 是5-HT4受体选择高亲和性激动剂,对5-HT4a和5-HT4b的 Ki 值分别为 2.5 和 8 nM。

产品描述

Prucalopride is a selective, high affinity 5-HT4 receptor agonist, inhibiting human 5-HT(4a) and 5-HT(4b) receptor with Ki value of 2.5 nM and 8 nM, respectively.

体外活性

Prucalopride induces contractions in a concentration-dependent manner with pEC50 of 7.5. Prucalopride (1 mM) significantly amplifies the rebound contraction of the guinea-pig proximal colon after electrical field stimulation. Prucalopride induces relaxation of the rat oesophagus preparation of rat oesophagus tunica muscularis mucosae with pEC50 of 7.8, yielding a monophasic concentration–response curve. [1] Prucalopride (0.1 μM) concentration-dependently increases the amplitude of submaximal cholinergic contractions and of acetylcholine release induced by electrical field stimulation in pig gastric circular muscle, and the effect is induced and enhanced IBMX (10 μM). [2] Prucalopride (1 μM) significantly enhances the electrically induced cholinergic contractions in pig descending colon, and the facilitating effect is significantly enhanced by Rolipram. [3]

体内活性

Prucalopride alters colonic contractile motility patterns in a dose-dependent fashion by stimulating high-amplitude clustered contractions in the proximal colon and by inhibiting contractile activity in the distal colon of fasted dogs. Prucalopride also causes a dose-dependent decrease in the time to the first giant migrating contraction (GMC); at higher doses of prucalopride, the first GMC generally occurres within the first half-hour after treatment. [4]

Cas No.

179474-85-2

分子式

C22H32ClN3O7

分子量

485.96

别名

琥珀酸普芦卡必利;R-108512;琥珀酸普卡比利;Resolor Succinate;Prucalopride Succinate

储存和溶解度

DMSO:90 mg/mL (185.2 mM)
H2O:89 mg/mL (183.1 mM)
Ethanol:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years