Description
Leukotriene B
4 (LTB
4) is a dihydroxy fatty acid derived from the 5-
lipoxygenase pathway of arachidonic acid metabolism and is an important mediator of the inflammatory process. The benzophenone dicarboxylic acid derivative LY223982 is a potent BLT
1 receptor antagonist. It inhibits the specific binding of radiolabeled-
LTB
4 to isolated human neutrophils with an IC
50 value of 13.2 nM. LY223982 inhibits the leukotriene B
4 (LTB
4)-
induced aggregation of guinea pig and human neutrophils with IC
50 values of 74 and 100 nM, respectively. However, concentrations of LY223982 up to 10 μM do not inhibit binding of LTB
4 to human BLT
1 or BLT
2 expressed in CHO cells.
References
[1] D. MARK GAPINSKI. Benzophenone dicarboxylic acid antagonists of leukotriene B4. 2. Structure-activity relationships of the lipophilic side chain[J]. Journal of Medicinal Chemistry, 1990, 33 10: 2807-2813. DOI:
10.1021/jm00172a020[2] W T JACKSON. Specific inhibition of leukotriene B4-induced neutrophil activation by LY223982.[J]. Journal of Pharmacology and Experimental Therapeutics, 1992, 263 3: 1009-1014.
[3] T. YOKOMIZO. Hydroxyeicosanoids Bind to and Activate the Low Affinity Leukotriene B4 Receptor, BLT2*[J]. The Journal of Biological Chemistry, 2001, 3 1: 12454-12459. DOI:
10.1074/jbc.m011361200
