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Biological Chemistry

Biochemical and Pharmacological Properties of 5-Lipoxygenase Inhibitor KF8940

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Pages 3131-3136 | Received 11 Jul 1988, Published online: 09 Sep 2014
 

Abstract

2-n-Heptyl-4-hydroxyquinoline-N-oxide (KF8940), isolated from Pseudomonas methanica, was a potent and selective inhibitor of the arachidonate 5-lipoxygenase of rat basophilic leukemia (RBL-1) cells. Kinetic analysis indicated that the inhibitory mode was non competitive. The Ki value was 3.5 × 10−7 m. KF8940 also inhibited 12-lipoxygenase of bovine platelets in a non-competitive manner, but with a Ki value of 7 × 10−5M. Ionophore A23187-stimulated SRS generation from rat peritoneal cells and antigen-stimulated SRS-A generation from sensitized rat lung were significantly inhibited by KF8940. KF8940 at a dose of 10 mg/kg (p.o.) suppressed the passive anaphylactic bronchoconstriction in guinea pigs.

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