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LY171883 is a selective, potent, orally active antagonist of the leukotriene D4 receptor.1 Dissociation constants (KB) for LY171883 on guinea pig ileum and parenchyma are 0.07 and 0.34 µM, respectively.1 LY171883 is an inhibitor of phosphodiesterase obtained from human polymorphonuclear leukocytes (IC50 of 22.6 µM) and various guinea pig tissues (IC50s range from 6.9-209 µM).1 At a concentration of 50-100 µM, LY171883 binds to the PPARγ nuclear receptor, inducing adipogenesis in cultured NIH3T3 fibroblasts.2,3
1
Fleisch, J.H., Rinkema, L.E., Haisch, K.D., et al. LY171883, 1-[2-hydroxy-3-propyl-4-[4-(1H-tetrazol-5-yl)butoxy]phenyl]ethanone, an orally active leukotriene D4 antagonist. J Pharmacol Exp Ther233148-157(1985).
2
Sala, A., Rossoni, G., Buccellati, C., et al. Formation of sulphidopeptide-leukotrienes by cell-cell interaction causes coronary vasoconstriction in isolated, cell-perfused heart of rabbit. Br J Pharmacol1101206-1212(1993).
3
Tontonoz, P., Hu, E., and Spiegelman, B.M. Stimulation of adipogenesis in fibroblasts by PPARγ2, a lipid-activated transcription factor. Cell791147-1156(1994).
Room temperature
in continental US; may vary elsewhere
SMILES
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CCCc1c(OCCCCc2nnn[nH]2)ccc(C(=O)C)c1O
Background Reading
Fleisch, J.H., Rinkema, L.E., Haisch, K.D., et al. LY171883, 1-[2-hydroxy-3-propyl-4-[4-(1H-tetrazol-5-yl)butoxy]phenyl]ethanone, an orally active leukotriene D4 antagonist. J Pharmacol Exp Ther233148-157(1985).
Tontonoz, P., Hu, E., and Spiegelman, B.M. Stimulation of adipogenesis in fibroblasts by PPARγ2, a lipid-activated transcription factor. Cell791147-1156(1994).
Sala, A., Rossoni, G., Buccellati, C., et al. Formation of sulphidopeptide-leukotrienes by cell-cell interaction causes coronary vasoconstriction in isolated, cell-perfused heart of rabbit. Br J Pharmacol1101206-1212(1993).
LY171883 is available in the following screening
library: