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  • Title: Characterization of CGS 8515 as a selective 5-lipoxygenase (5-LO) inhibitor.
    Author: Ku EC, Raychaudhuri A, Ghai G, Kimble EF, Lee WH, Colombo C, Dotson R, White D, Oglesby TD, Wasley JW.
    Journal: Adv Prostaglandin Thromboxane Leukot Res; 1989; 19():86-9. PubMed ID: 2526568.
    Abstract:
    1. CGS 8515 selectively inhibited 5-LO (IC50 = 0.1 microM) with negligible effect on CO, 12-LO, 15-LO and TxS at concentrations up to 100 microM. 2. CGS 8515 selectively inhibited A23187-induced formation of 5-LO products in rat and human whole blood with a 20-70 fold separation of effects over the formation of CO products. 3. Ex vivo and in vivo studies with rats showed that CGS 8515, at an oral dose of 2-50 mg/kg, significantly inhibited A23187-induced formation of LTs in whole blood and in the lung. The effect persisted for at least 6 h in the ex vivo blood model. 4. CGS 8515, at oral doses as low as 5 mg/kg, significantly suppressed exudate volume and leukocyte migration in the carrageenan-induced pleurisy and sponge models in the rat.
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