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The 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.

japanese journal of pharmacology/japanese journal of pharmacology

Effects of l-[(2-Thiazolin-2-yl)amino]acetyl-4-(l,3-dithiol-2-ylidene)-2,3,4,5-tetrahydro-1H-1-benzazepin-3,5-dione Hydrochloride (KF-14363) on Active Oxygen Production