112727-80-7

112727-80-7 structure

Name: Renzapride
Chemical Name: 4-amino-N-(1-azabicyclo[3.3.1]nonan-4-yl)-5-chloro-2-methoxybenzamide
CAS Number: 112727-80-7
Molecular Formula: C₁₆H₂₂ClN₃O₂
Molecular Weight: 323.81800
Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
Create Date: 2018-04-20 08:00:00
Modify Date: 2024-01-10 15:25:03
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[1]. Renzapride could be used for constipation predominant irritable bowel syndrome (C-IBS) study[2].

Name	4-amino-N-(1-azabicyclo[3.3.1]nonan-4-yl)-5-chloro-2-methoxybenzamide
Synonyms	MK-0646 Renzaprida Renzapride Renzapridum

Description	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[1]. Renzapride could be used for constipation predominant irritable bowel syndrome (C-IBS) study[2].
Related Catalog	Research Areas >> Metabolic Disease Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor
Target	5-HT4 Receptor:115 nM (Ki)
In Vitro	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[3].
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 a 51Cr-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 a 51Cr-labeled liquid meal from the murine stomach.
References	[1]. Camilleri M, et al. Effect of renzapride on transit in constipation-predominant irritable bowel syndrome. Clin Gastroenterol Hepatol. 2004;2(10):895-904. [2]. Scarpellini E, et al. Renzapride: a new drug for the treatment of constipation in the irritable bowel syndrome. Expert Opin Investig Drugs. 2008;17(11):1663-1670. [3]. Nagakura Y, et al. Pharmacological properties of a novel gastrointestinal prokinetic benzamide selective for human 5-HT4 receptor versus human 5-HT3 receptor. Pharmacol Res. 1999;39(5):375-382. [4]. Mawe GM, et al. Blockade of 5-HT-mediated enteric slow EPSPs by BRL 24924: gastrokinetic effects. Am J Physiol. 1989;257(3 Pt 1):G386-G396.

Density	1.3g/cm3
Boiling Point	469.2ºC at 760mmHg
Molecular Formula	C₁₆H₂₂ClN₃O₂
Molecular Weight	323.81800
Flash Point	237.6ºC
Exact Mass	323.14000
PSA	67.59000
LogP	3.05490
Vapour Pressure	5.6E-09mmHg at 25°C
Index of Refraction	1.614