Alterations in the distribution and orexigenic effects of dexamethasone in CAR-null mice

Pharmacol Biochem Behav. 2004 Jun;78(2):285-91. doi: 10.1016/j.pbb.2004.04.001.

Abstract

The constitutive androstane receptor (CAR, NR1I3) has emerged as an important regulator of drug metabolism. CAR responds to a wide spectrum of xenobiotics by inducing expression of cytochrome P450 (CYP) enzymes and a number of other proteins responsible for drug metabolism in the liver. The xenosensor function of CAR overlaps with that of the pregnane X receptor (PXR), another xenobiotic receptor that belongs to the nuclear hormone superfamily. We observed that injection of dexamethasone (Dex), a ligand for the glucocorticoid receptor (GR) and PXR but not CAR, results in an unexpected twofold increase in the stomach weight of CAR-null animals relative to wild-type animals. Here, we show that CAR knockout mice have elevated levels of Dex in the brain, resulting in a more rapid and robust increase in the hypothalamic expression of the GR-responsive target genes encoding neuropeptide Y (NPY) and neuropeptide Y receptor subtype 1 (NPY-R1). As expected, this is accompanied by a higher increase in the food intake of the CAR-null animals. The data described here highlight the complexity of the overlapping functions of CAR and PXR.

Publication types

  • Comparative Study
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Body Weight / drug effects
  • Body Weight / genetics
  • Constitutive Androstane Receptor
  • Dexamethasone / pharmacokinetics*
  • Dexamethasone / pharmacology*
  • Male
  • Mice
  • Mice, Knockout
  • Neuropeptide Y / biosynthesis
  • Neuropeptide Y / genetics
  • Organ Size / drug effects
  • Organ Size / genetics
  • Receptors, Cytoplasmic and Nuclear / biosynthesis
  • Receptors, Cytoplasmic and Nuclear / deficiency*
  • Receptors, Cytoplasmic and Nuclear / genetics*
  • Receptors, Neuropeptide Y / biosynthesis
  • Receptors, Neuropeptide Y / genetics
  • Stomach / drug effects
  • Stomach / physiology
  • Transcription Factors / biosynthesis
  • Transcription Factors / deficiency*
  • Transcription Factors / genetics*

Substances

  • Constitutive Androstane Receptor
  • Neuropeptide Y
  • Nr1i3 protein, mouse
  • Receptors, Cytoplasmic and Nuclear
  • Receptors, Neuropeptide Y
  • Transcription Factors
  • neuropeptide Y-Y1 receptor
  • Dexamethasone