Leucine thiorphan is an inhibitor of enkephalinase.

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.

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.