INDUCTION OF CYP1A1 BY GABA RECEPTOR LIGANDS

The induction of CYP1A1 is mediated via the aromatic hydrocarbon (Ah) receptor. Studies from our laboratory show CYP1A1 induction by picroto xin and phenobarbital which prompted us to examine if other ligands of the gamma-aminobutyric acid (GABA) receptor could also induce CYP1A1. Here we report the nuclear translocation of the Ah receptor and its D NA binding activity to radiolabeled double-stranded synthetic xenobiot ic response elements (XREs) in nuclear extracts, increased accumulatio n of CYP1A1 mRNA, and alterations in intracellular calcium concentrati ons in cells exposed to GABA receptor ligands. (C) 1996 Academic Press , Inc.