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].
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.