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Effects of 1-[(2-thiazolin-2-yl)amino]acetyl-4-(1,3-dithiol-2-ylidene)- 2,3,4,5-tetrahydro-1H-1-benzazepin-3,5-dione hydrochloride (KF-14363) on active oxygen production.

AbstractThe effects of KF-14363 on active oxygen production and membrane stabilization were studied. KF-14363 did not affect hypotonic hemolysis (10% and 70%) and did not inhibit lipid peroxide production induced by t-butyl hydroperoxide at concentrations of less than 100 microM. KF-14363 significantly inhibited active oxygen production in peritoneal exudate cells (PEEC) stimulated with arachidonic acid, A23187 and carbon tetrachloride (CCl4) at concentrations over 10 microM, 100 microM and 1 microM, respectively. It tended to inhibit formyl-methionyl-leucyl-phenylalanine-stimulated production of active oxygen in PEEC at concentrations over 10 microM, but there was no significant difference owing to large dispersion. Superoxide dismutase (SOD, 10(4) U/ml) significantly inhibited CCl4-stimulated production of active oxygen in PEEC. KF-14363 inhibited the radical production from CCl4 in the presence of a 9000 x g supernatant fraction of the rat liver which was administered with enzyme induction compounds (S9 mix). SOD (10(4) U/ml) was not effective in this system. In conclusion, KF-14363 inhibited active oxygen production in PEEC induced by various stimulants and also the radical formation from CCl4 in the presence of S9 mix solution.
AuthorsI Yoshitake, K Kubo (Affiliation: Pharmaceutical Research Laboratories, Kyowa Hakko Kogyo Co., Ltd., Shizuoka, Japan.)
JournalJapanese journal of pharmacology (Jpn J Pharmacol) Vol. 57 Issue 2 Pg. 137-45 (Oct 1991) ISSN: 0021-5198 JAPAN
PMID1812295 (Publication Type: Journal Article)
Chemical References
  • Benzazepines
  • Biological Factors
  • Free Radicals
  • Lipid Peroxides
  • Thiazoles
  • KF 14363
  • Carbon Tetrachloride
  • Oxygen
Topics
  • Animals
  • Ascitic Fluid (cytology, metabolism)
  • Benzazepines (therapeutic use)
  • Biological Factors (pharmacology)
  • Carbon Tetrachloride (metabolism)
  • Erythrocyte Membrane (drug effects)
  • Erythrocytes (drug effects, metabolism)
  • Free Radicals
  • Lipid Peroxidation (drug effects)
  • Lipid Peroxides (biosynthesis)
  • Liver (drug effects, metabolism)
  • Liver Diseases (metabolism, prevention & control)
  • Male
  • Oxygen (metabolism)
  • Rats
  • Rats, Inbred Strains
  • Thiazoles (therapeutic use)