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• W2000901498 abstract "2,4,6,8- and 1,3,6,8-tetrachlorodibenzofuran (TCDF) competitively displace [3H]2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) from the rat cytosolic receptor protein and their EC50 values were 1.5 × 10−6 and 1.25 x 10−7 M, respectively. In contrast to their relatively high binding avidities these TCDF isomers were poor inducers of benzo[a]pyrene hydroxylase and ethoxyresorufin O-deethylase in rat hepatoma H-4-II E cells in culture (EC50 > 10−5 M). Coadministration of different concentrations of 2,4,6,8- and 1,3,6,8-TCDF (10−5, 10−6 and 10−7 M) with 2 × 10−10 M, 2,3,7,8-TCDD (a dose which elicits 80% of the maximal induction response) resulted in significant decreases in the expected (additive) induction of benzo[a]pyrene hydroxylase and ethoxyresorufin O-deethylase by the mixture. Thus the partial agonists, 1,3,6,8- and 2,4,6,8-TCDF, antagonize the receptor-mediated enzyme induction activity of 2,3,7,8-TCDD presumably via competitive displacement of 2,3,7,8-TCDD from the receptor protein. In contrast, coadministration of 2,3,7,8-TCDF and 2,3,7,8-TCDD gave additive enzyme induction responses. The identification of the 2,3,7,8-TCDD antagonists represents a new class of halogenated aryl hydrocarbons." @default.
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• W2000901498 date "1986-05-01" @default.
• W2000901498 modified "2023-10-15" @default.
• W2000901498 title "Polychlorinated dibenzofurans as 2,3,7,8-tcdd antagonists: In vitro inhibition of monooxygenase enzyme induction" @default.
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• W2000901498 doi "https://doi.org/10.1016/0378-4274(86)90009-3" @default.
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