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| | Renzapride Basic information |
| Product Name: | Renzapride | | Synonyms: | Renzapride;4-amino-N-[(4R,5S)-1-azabicyclo[3.3.1]nonan-4-yl]-5-chloro-2-methoxybenzamide;Benzamide, 4-amino-N-(1R,4S,5R)-1-azabicyclo[3.3.1]non-4-yl-5-chloro-2-methoxy-, rel-;Renzapridum;BRL-24924A;program AZM-112 | | CAS: | 112727-80-7 | | MF: | C16H22ClN3O2 | | MW: | 323.82 | | EINECS: | | | Product Categories: | API | | Mol File: | 112727-80-7.mol |  |
| | Renzapride 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 |
| | Renzapride 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.
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| 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 |
| | Renzapride Preparation Products And Raw materials |
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