Renzapride

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Renzapride

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。

CAS NO:

112727-80-7

BRL 24924

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。

生物活性

Renzapride (BRL 24924), a substituted benzamide, is a full5-HT₄receptoragonist with aK_ivalue of 115 nM. Renzapride (BRL 24924) is also a5HT2band5HT3 receptorantagonist^[1]. Renzapride could be used for constipation predominant irritable bowel syndrome (C-IBS) study^[2].

IC₅₀& Target^[1]

5-HT₄Receptor

115 nM (Ki)

体外研究
(In Vitro)

Renzapride replaces specific binding of [H³] GR 113808 (a selective 5-HT receptor antagonist) to cloned human 5-HT₄receptors with a K_ivalue of 115 nM^[3].

体内研究
(In Vivo)

Renzapride (BRL 24924) (100 μg i.v.) results in a partial reverse of both the delayed solid and liquid meals emptying^[2].
Renzapride (BRL 24924) (0.5-1 mg/kg) significantly increases the rate of emptying of a⁵¹Cr-labeled liquid meal from the murine stomach^[4].

Animal Model:	Dog (simulating gastroparesis)^[2]
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)^[2]
Dosage:	0.5-1 mg/kg
Administration:	p.o.
Result:	Significantly increase the rate of emptying of a⁵¹Cr-labeled liquid meal from the murine stomach.

Clinical Trial

分子量

323.82

性状

Solid

Formula

C₁₆H₂₂ClN₃O₂

CAS 号

112727-80-7

中文名称

伦扎必利

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month