The endogenous substrates of brain CYP2D

Eur J Pharmacol. 2014 Feb 5;724:211-8. doi: 10.1016/j.ejphar.2013.12.025. Epub 2013 Dec 24.


CYP2D6, one of the major cytochrome P450 isoforms present in the human brain, is associated with the incidence and prevalence of central nervous system (CNS) diseases. Human CYP2D6 and rat CYP2D are involved in the metabolism of various neurotransmitters and neurosteroids. Brain CYP2D can be regulated by endogenous steroids, including sex hormones. The alteration of CYP2D-mediated metabolism induced by endogenous steroids may cause changes in sensitivity to environmental and industrial toxins and carcinogens as well as physiological and pathophysiological processes controlled by biologically active compounds. This review summarizes the current knowledge regarding the distribution, endogenous substrates, and regulation of brain CYP2D.

Keywords: Brain; Cytochrome P450 2D; Endogenous substrates.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Alcohol Oxidoreductases / metabolism
  • Animals
  • Aryl Hydrocarbon Hydroxylases / metabolism
  • Brain / metabolism*
  • Cytochrome P-450 CYP2D6 / metabolism*
  • Cytochrome P-450 Enzyme System / metabolism
  • Cytochrome P450 Family 2
  • Humans


  • Cytochrome P-450 Enzyme System
  • Cyp2d3 protein, rat
  • Alcohol Oxidoreductases
  • Aryl Hydrocarbon Hydroxylases
  • Cyp2d1 protein, rat
  • Cyp2d2 protein, rat
  • Cyp2d4 protein, rat
  • Cytochrome P-450 CYP2D6
  • Cytochrome P450 Family 2