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Renzapride

Product NameRenzapride
CAS112727-80-7
MFC16H22ClN3O2
MW323.82
EINECS
MOL File112727-80-7.mol

Chemical Properties

Melting point	>260°
Boiling point	469.2±45.0 °C(Predicted)
Density	1.30±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
pka	13.59±0.20(Predicted)
form	Solid
color	White to off-white

Usage And Synthesis

Uses

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].

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.

IC 50

5-HT₄ Receptor: 115 nM (Ki)

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. DOI:10.1016/s1542-3565(04)00391-x
[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. DOI:10.1517/13543784.17.11.1663
[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. DOI:10.1006/phrs.1998.0454
[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. DOI:10.1152/ajpgi.1989.257.3.G386

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