CHLORINATED TRANS STILBENES - COMPETITIVE-BINDING TO THE AH RECEPTOR, INDUCTION OF CYTOCHROME-P-450 MONOOXYGENASE ACTIVITY AND PARTIAL 2,3,7,8-TCDD ANTAGONISM uri icon

abstract

  • Chlorinated trans stilbenes bind with high affinity to the cytosolic Ah receptor from Wistar rat liver. The EC50values for competition with [3H]-2, 3, 7, 8-tetrachlorodibenzo-p-dioxin (TCDD) cover a range from 10400 nM, but with no apparent relationship between molecular structure and binding activity. These compounds induce monooxygenase enzyme activity in rat hepatoma H-4-II E cells in culture only weakly, again with no apparent dependence on molecular structure, and the weakest enzyme inducers act as antagonists for the induction of these enzymes by TCDD. In vivo administration of 3, 3, 4, 4-tetrachloro-trans-stilbene in the rat leads to decreased Ah receptor levels. 1990, Taylor & Francis Group, LLC. All rights reserved.

published proceedings

  • TOXICOLOGICAL AND ENVIRONMENTAL CHEMISTRY

author list (cited authors)

  • BUNCE, N. J., LANDERS, J. P., SCHNEIDER, U. A., SAFE, S. H., & ZACHAREWSKI, T. R.

citation count

  • 9

complete list of authors

  • BUNCE, NJ||LANDERS, JP||SCHNEIDER, UA||SAFE, SH||ZACHAREWSKI, TR

publication date

  • August 1990