In vivo 'enkephalinase' inhibition by acetorphan in human plasma and CSF

Eur J Pharmacol. 1986 Jun 5;125(1):147-50. doi: 10.1016/0014-2999(86)90094-4.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acids, Sulfur / pharmacology*
  • Endopeptidases / blood
  • Endopeptidases / cerebrospinal fluid
  • Humans
  • Neprilysin
  • Peptidyl-Dipeptidase A / blood
  • Protease Inhibitors*
  • Thiorphan* / analogs & derivatives*
  • Tiopronin / analogs & derivatives
  • Tiopronin / pharmacology*

Substances

  • Amino Acids, Sulfur
  • Protease Inhibitors
  • racecadotril
  • Thiorphan
  • Tiopronin
  • Endopeptidases
  • Peptidyl-Dipeptidase A
  • Neprilysin