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.

Information

Prucalopride (R-93877) is a selective, high affinity 5-HT receptor agonist for5-HT4Aand5-HT4Breceptor withKiof 2.5 nM and 8 nM, respectively, exhibits >290-fold selectivity against other 5-HT receptor subtypes.
In vitro

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.

In vivo

Complete bowel movements per week is 30.9% of those receiving 2 mg of Prucalopride and 28.4% of those receiving 4 mg of Prucalopride, as compared with 12.0% in the placebo group. 47.3% of patients receiving 2 mg of Prucalopride and 46.6% of those receiving 4 mg of Prucalopride has an increase in the number of spontaneous, complete bowel movements of one or more per week, on average, as compared with 25.8% in the placebo group. Prucalopride (2 mg or 4 mg) significantly improves all other secondary efficacy end points, including patients\' satisfaction with their bowel function and treatment and their perception of the severity of their constipation symptoms. Prucalopride (4 mg daily) accelerates overall gastric emptying and small bowel transit in patients with constipation without a rectal evacuation disorder. Prucalopride (4 mg daily) tends to accelerate overall colonic transit with significantly faster overall colonic transit and ascending colon emptying. Higher proportions of patients on prucalopride 2 mg (19.5%), 4 mg (23.6%) has three or more spontaneous complete bowel movements(SCBM)/week compared with placebo (9.6%). Prucalopride also significantly improves secondary efficacy and quality of life endpoints, including the proportion of patients with an increase of one or more SCBM/week, evacuation completeness, perceived disease severity and treatment effectiveness and quality of life. 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.
Cell Data

cell lines：A.E7 or Th17 cells

Concentrations：

Incubation Time：

Powder Purity:≥99%

规格

别名

普卡必利

英文别名

R-93877 | 7-Benzofurancarboxamide, 4-amino-5-chloro-2,3-dihydro-N-[1-(3-methoxypropyl)-4-piperidinyl]-

规格或纯度

Moligand™, 10mM in DMSO

英文名称

Prucalopride

生化机理

普卡必利（R-93877）是一种选择性高亲和力 5-HT 受体激动剂，对 5-HT4A 和 5-HT4B 受体的_Ki分别为 2.5 nM 和 8 nM，对其他 5-HT 受体亚型的选择性大于 290 倍。

储存条件

-80℃储存

运输条件

特低温运输

作用类型

激动剂

作用机制

羟色胺 4 (5-HT4) 受体激动剂

名称和识别符

EC号

878-837-3

分子类型

小分子

Isomeric SMILES

COCCCN1CCC(CC1)NC(=O)C2=CC(=C(C3=C2OCC3)N)Cl

分子量

367.87

Reaxy-Rn

8357099

Reaxys-RN link address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=8357099&ln=

技术文档

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高级数据

产品属性

ALogP	2

关联靶点（人）

HTR4 Tclin 5-羟色胺受体 4(5-hydroxytryptamine receptor 4) (5 活性数据)

点击查看靶蛋白信息： HTR4

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

HTR3A Tclin 5-羟色胺受体 3A(5-hydroxytryptamine receptor 3A) (1 活性数据)

点击查看靶蛋白信息： HTR3A

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

化学和物理性质

溶解性

Solubility (25°C) In vitro DMSO: 42 mg/mL (197.89 mM); Ethanol: 5 mg/mL (23.55 mM); Water: Insoluble;

熔点

92 °C

质检证书（CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):

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溶液计算器

摩尔浓度计算器

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质量

浓度

体积

分子量

g/mol

稀释计算器

计算配制储备溶液所需的稀释度。

浓度1（C1）

体积 1 (V1)

浓度 2 (C2)

体积 2 (V2)

复溶计算器

复溶计算器允许您快速计算试剂的体积，以复溶小瓶。只需输入试剂的质量和目标浓度，计算器将确定其余部分。

体积（添加到小瓶中）

质量（小瓶）

所需的复溶浓度

常见问题

如何获取批次专用COA？

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「Moligand?」是什么？

「Moligand?」是阿拉丁科学的高端产品线之一，专为多个工作流程中的高纯度应用而设计。与同类工作流程中的标准级别相比，「Moligand?」产品通常具有更严格的规格、更严谨的 QC 以及更强的批间一致性。

本产品应如何储存？

请于?80 °C条件下保存。需超低温保存以维持规定的有效期。

本产品如何运输？

本产品采用干冰配冷袋冷冻运输。收货后请立即拆包，并按上述储存条件保存；处理干冰时请戴隔热手套并保持通风。

本产品的 CAS 号、分子式和分子量是多少？

本产品的 CAS 号为 179474-81-8，分子式为 C18H26ClN3O3，分子量为 367.87 g/mol。

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