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KMID : 0369319940140020184
Allergy
1994 Volume.14 No. 2 p.184 ~ p.195
In Vitro Difference of PAF-receptor Antagonisis CV-6209, WEB 2086 on the PAF-induced Eosinophil Chemotaxis and Activation in asthmatics


Abstract
Nowadays because of the role of PAF especially focusing non-specific bronchial hypereresponsiveness(NSBH) which is the fundamental characteristics of asthma, anti PAF agents are under investigation. In this study, the effect of PAF receptor
antagonists,
structural PAF analygue CV-6209, structurally not related agent WEB 2086 on PAF-induced eosinophil chemotaxis by Boyden chamber method and activation process, at membrane LTC4 generation and eosinophil cationic protein(ECP) by the process of
degranulation by RIA were done. The difference in the potency of both Anti-PAF agents on PAF-induced eosinophil chemotaxis(10E-8M) and the process of activation(10E-7M) were compared by the subtracted ID50, concentration producing 50% inhibition,
to
find the possibility of these agents as anti-asthmatics.
@ES The results were as follows:
@EN 1) ID50 of CV, WEB on eosinophil chemotaxis were 1.32¡¾0.43¡¿10E-7, 1.87¡¾0.56¡¿10E-7 respectively.
2) ID50 on LTC4 production of CV, WEB, were 1.38¡¾0.36¡¿10E-6, 1.36¡¾0.34¡¿10E-6, and these were less potent than chemotaxis (P=0.024).
3) ID50 on ECP release of CV, WEB were 3.2¡¾0.56¡¿10E-6, 1.6¡¾0.32¡¿10E-6, and also less potent than chemotaxis(P=0.037).
From these results we documented PAF infiltrated and activated eosinophil in vitro, and also PAF receptor antagonist, CV-6209, WEB 2086 inhibited PAF-induced not only eosinophol chemotaxis but activation, we speculate these agent might inhibit
NSBR
through these actions in vivo and in near future expect these agents clinical trial as anti-asthma drug.
KEYWORD
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