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Leukotriene B4 (LTB4) is a dihydroxy fatty acid derived from arachidonic acid through the 5-lipoxygenase pathway.1,2 It promotes a number of leukocyte functions including aggregation, stimulation of ion fluxes, enhancement of lysosomal enzyme release, superoxide anion production, chemotaxis, and chemokinesis.3,4 At least two LTB4 receptors, termed BLT1 and BLT2, have been identified. 14,15-dehydro LTB4 is a LTB4 receptor antagonist that has a higher binding affinity for BLT1, demonstrating a Ki value of 27 nM, compared to BLT2, which has a Ki value of 473 nM.5 14,15-dehydro LTB4 inhibits LTB4-induced release of lysozymes from rat polymorphonuclear leukoctyes with an IC50 value of 1 µM.6
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1
Rådmark, O., Malmsten, C., Samuelsson, B., et al. Leukotriene A: Stereochemistry and enzymatic conversion to leukotriene B. Biochem Biophys Res Commun 92 954-961 (1980).
2
McGee, J., Fitzpatrick, F. Enzymatic hydration of leukotriene A4. J Biol Chem 260 12832-12837 (1985).
3
Ford-Hutchinson, A.W. Leukotriene B4 in inflammation. Crit Rev Immunol 10 1-12 (1990).
4
McMillan, R.M., Foster, S.J. Leukotriene B4 and inflammatory disease. Agents Actions 24 114-119 (1988).
5
Wang, S., Gustafson, E., Pang, L., et al. A novel hepatointestinal leukotriene B4 receptor. J Biol Chem 275 40686-40694 (2000).
6
Shimazaki, T., Kobayashi, Y., Sato, F., et al. Some newly synthesized leukotriene B4 analogs inhibit LTB4-induced lysozyme release from rat polymorphonuclear leukocytes. Prostaglandins 39 459-467 (1990).
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