| Bioactivity | Racecadotril (Acetorphan) is a neutral endopeptidase (NEP) inhibitor. Racecadotril and its active metabolite Thiorphan inhibits purified NEP activity from mouse brain with Kis of 4500 and 6.1 nM, , respectively. Antidiarrheal agent[1]. | ||||||||||||
| In Vivo | In mice, following i.v. administration, Racecadotril is rapidly metabolized to Thiorphan; thus, 30 min after the injection only Thiorphan is recovered from the kidney whereas the parent compound Racecadotril is not detected[1]. In rats 92% of a single-dose (10 mg/kg) of radioactively labeled Racecadotril is eliminated within 24 h[1].Racecadotril is a neutral endopeptidase (NEP) inhibitor with known antidiarrheal activity in animals. Orally administered Racecadotril (100 mg/kg ) shows efficacy in a rat model of castor oil-induced diarrhea[2]. Animal Model: | ||||||||||||
| Name | Racecadotril | ||||||||||||
| CAS | 81110-73-8 | ||||||||||||
| Formula | C21H23NO4S | ||||||||||||
| Molar Mass | 385.48 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Marion Eberlin, et al. A comprehensive review of the pharmacodynamics, pharmacokinetics, and clinical effects of the neutral endopeptidase inhibitor Racecadotril. Front Pharmacol. 2012 May 30;3:93. [2]. David W Griggs, et al. Pharmacologic Comparison of Clinical Neutral Endopeptidase Inhibitors in a Rat Model of Acute Secretory Diarrhea. J Pharmacol Exp Ther. 2016 May;357(2):423-31. |
Racecadotril
CAS: 81110-73-8 F: C21H23NO4S W: 385.48
Racecadotril (Acetorphan) is a neutral endopeptidase (NEP) inhibitor. Racecadotril and its active metabolite Thiorphan i
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