title: In vivo 'enkephalinase' inhibition by acetorphan in human plasma and CSF.
abstract: Thiorphan, the potent inhibitor of 'enkephalinase', has shown some analgesic properties in experimental animals and in man. The possibility that the intravenous infusion of acetorphan, a prodrug of thiorphan (26 micrograms/kg per min for 60 min), can inhibit plasma and cerebrospinal fluid (CSF) enkephalinase in man in vivo was investigated. A decrease of approximately 65% in enzyme activity was observed in both plasma and CSF. Acetorphan did not induce any significant variation of plasma angiotensin-converting enzyme activity.
mesh_terms: D000603:Amino Acids, Sulfur / Q000494:pharmacology*; D010450:Endopeptidases / Q000097:blood / Q000134:cerebrospinal fluid; D006801:Humans; D015260:Neprilysin; D007703:Peptidyl-Dipeptidase A / Q000097:blood; D011480:Protease Inhibitors; D015244:Thiorphan / Q000031:analogs & derivatives*; D008625:Tiopronin / Q000031:analogs & derivatives / Q000494:pharmacology*
chemical_list: D000603:Amino Acids, Sulfur; D011480:Protease Inhibitors; C049331:racecadotril; D015244:Thiorphan; D008625:Tiopronin; D010450:Endopeptidases; D007703:Peptidyl-Dipeptidase A; D015260:Neprilysin