thiorphan

Thiorphan is an neprilysin inhibitor (NEP; IC50 : 0.007 μM).

Thiorphan disulfide is an impurity of Racecadotril -- an antidiarrheal and enkephalinase inhibitor that reduces the amount of water and electrolytes absorbed into the intestine.

Leucine thiorphan is an inhibitor of enkephalinase.

Azidothiorphan is a photoaffinity ligand for the active site of the neutral endopeptidase 24.11. After ultraviolet irradiation the inhibitor binds irreversibly to the enzyme, and photolabeling occurs at the active site. The competitive inhibitor thiorphan protects the endopeptidase from inactivation.

Racecadotril (Acetorphan) has been investigated for the basic science and treatment of Diarrhea, Acute Diarrhea, and Acute Gastroenteritis.

Dexecadotril is a powerful and selective neprilysin inhibitor. It behaves as a prodrug of the enantiomer of thiorphan.

Racecadotril-d5 is intended for use as an internal standard for the quantification of racecadotril by GC- or LC-MS. Racecadotril is a prodrug form of the neprilysin (NEP) inhibitor thiorphan. In vivo, racecadotril reduces or prevents castor oil-induced diarrhea without delaying intestinal transit in rats when administered at doses of 80 or 100 mg kg, respectively. It also decreases the duration of diarrhea and increases body weight gain in a neonatal gnotobiotic pig model of human rotavirus-induced diarrhea. Formulations containing racecadotril have been used in the treatment of acute diarrhea.