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Abstract

Specific inhibition of leukotriene B4-induced neutrophil activation by LY223982.

W T Jackson, R J Boyd, L L Froelich, B E Mallett and D M Gapinski
Journal of Pharmacology and Experimental Therapeutics December 1992, 263 (3) 1009-1014;
W T Jackson
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R J Boyd
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L L Froelich
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B E Mallett
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D M Gapinski
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Abstract

LY223982, (E)-5-(3-carboxybenzoyl)-2-((6-(4-methoxyphenyl)-5- hexenyl)oxy)benzenepropanoic acid, is a newly discovered potent inhibitor of specific binding of leukotriene B4 (LTB4) to its receptor on human neutrophils. This study demonstrated that the compound is also a specific antagonist of LTB4-induced neutrophil activation under both in vitro and in vivo conditions. LY223982 was found to be 189-fold more effective in displacing [3H]LTB4 than 35S-N-formyl-L-methionyl-L-leucyl-L-phenylalanine (FMLP) from their corresponding receptors on human neutrophils. The concentration inhibiting 50% of response (IC50) for displacement of [3H]LTB4 (13.2 nM) was only 6.8-fold higher than the value for nonradioactive LTB4. The compound inhibited the aggregation of guinea pig neutrophils caused by LTB4 more strongly than FMLP or platelet-activating factor. The IC50 for inhibition of LTB4-induced responses (74 nM) was 93- and > 135-fold lower than the IC50 for inhibition of the corresponding FMLP and platelet-activating factor-induced effects. LY223982 was also a potent antagonist of the aggregation of human neutrophils by LTB4 (IC50, 100 nM). Chemotaxis of human neutrophils induced by LTB4 was only modestly inhibited by the compound (IC50 = 6 microM) but it had even less effect on cell movement caused by FMLP. LY223982 inhibited transient leukopenia induced in rabbits with LTB4 (ED50, 3 mg/kg) but not with FMLP. It had no agonist activity in any of the test systems. In summary, the results indicate that LY223982 is a potent specific antagonist of LTB4-induced neutrophil activation.

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Journal of Pharmacology and Experimental Therapeutics
Vol. 263, Issue 3
1 Dec 1992
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Abstract

Specific inhibition of leukotriene B4-induced neutrophil activation by LY223982.

W T Jackson, R J Boyd, L L Froelich, B E Mallett and D M Gapinski
Journal of Pharmacology and Experimental Therapeutics December 1, 1992, 263 (3) 1009-1014;

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Abstract

Specific inhibition of leukotriene B4-induced neutrophil activation by LY223982.

W T Jackson, R J Boyd, L L Froelich, B E Mallett and D M Gapinski
Journal of Pharmacology and Experimental Therapeutics December 1, 1992, 263 (3) 1009-1014;
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