Renzapride

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].

Research Areas >> Metabolic Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

5-HT4 Receptor:115 nM (Ki)

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].

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.

[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.