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.
体内研究
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.
In rats 92% of a single-dose (10 mg/kg) of radioactively labeled Racecadotril is eliminated within 24 h.
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.
Animal Model:
6-to-7-week-old male Wistar rats
Dosage:
100 mg/kg
Administration:
A single oral treatment; 30 minutes before castor oil administration.
Result:
Significantly reduced stool output but did not prevent the occurrence of diarrhea (100% incidence).
分子式
C21H23NO4S
分子量
385.48
CAS号
81110-73-8
中文名称
消旋卡多曲
运输条件
Room temperature in continental US; may vary elsewhere.