Renzapride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Renzapride (BRL 24924)，是一种取代苯甲酰胺，是 5-HT4 受体激动剂，也是 5HT2b 和 5HT3 受体拮抗剂。Renzapride (BRL 24924) 可以用于便秘型肠易激综合征 (C-IBS) 的研究。

Renzapride (BRL 24924), a substituted benzamide, is a full 5-HT4 receptor agonist with a Ki value of 115 nM. Renzapride (BRL 24924) is also a 5HT2b and 5HT3 receptor antagonist. Renzapride could be used for constipation predominant irritable bowel syndrome (C-IBS) study.

Renzapride replaces specific binding of [H3] GR 113808 (a selective 5-HT receptor antagonist) to cloned human 5-HT4 receptors with a Ki value of 115 nM.

Renzapride (BRL 24924) (100 μg i.v.) results in a partial reverse of both the delayed solid and liquid meals emptying.Renzapride (BRL 24924) (0.5-1 mg/kg) significantly increases the rate of emptying of a 51Cr-labeled liquid meal from the murine stomach.Animal Model:Dog (simulating gastroparesis)Dosage:100 μg/kg Administration:i.v.Result:Results in a partial reverse of both the delayed solid and liquid meals emptying.Animal Model: Mice (30-45g) Dosage:0.5-1 mg/kg Administration:p.o.Result:Significantly increase the rate of emptying of a 51Cr-labeled liquid meal from the murine stomach.

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GPCR/G Protein

5-HT Receptor

5-HT Receptor

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112727-80-7

323.82

C16H22ClN3O2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 25 mg/mL (77.20 mM; 超声助溶 )

COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN2CCC[C@@H]1C2

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(-20℃)

With Ice Pack

≥ 2 years