Inhibitory effect of econazole on the release of thromboxanes.
The effect of econazole on the release of thromboxanes was investigated. It was found that econazole inhibited concentration-dependently the aggregation of guinea pig platelets stimulated with arachidonic acid. The compound also reduced significantly the LTB4-induced contraction of guinea pig lung parenchyma strips and the contraction of rabbit aorta to the effluent of LTD4-stimulated guinea pig lungs, both effects mediated mostly by thromboxane generation. The concentration of TXB2 in the effluents from LTD4 stimulated lungs, assayed by EIA, was significantly reduced following pretreatment of the lungs with 10(-4) M and 10(-5) M of econazole, whereas the levels of PGE2 were increased. These results demonstrate that econazole is a selective inhibitor of thromboxane synthesis.
Jancar
S
S
Departamento de Imunologia, Universidade de São Paulo, Brasil.
Teixeira
C F
CF
de Lima
W T
WT
Fujimura
A Y
AY
Sirois
P
P
D000818:Animals; D001011:Aorta / Q000187:drug effects / Q000502:physiology; D016718:Arachidonic Acid / Q000494:pharmacology; D015232:Dinoprostone / Q000378:metabolism; D004464:Econazole / Q000494:pharmacology*; D006168:Guinea Pigs; D007975:Leukotriene B4 / Q000494:pharmacology; D008168:Lung / Q000187:drug effects / Q000502:physiology; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000494:pharmacology; D011817:Rabbits; D013189:SRS-A / Q000494:pharmacology; D013929:Thromboxane B2 / Q000378:metabolism; D013931:Thromboxanes / Q000502:physiology*
D010975:Platelet Aggregation Inhibitors; D013189:SRS-A; D013931:Thromboxanes; D007975:Leukotriene B4; D016718:Arachidonic Acid; D013929:Thromboxane B2; D004464:Econazole; D015232:Dinoprostone