Cytochrome P450 enzymes in the brain: emerging evidence of biological significance

Trends Pharmacol Sci. 2011 Dec;32(12):708-14. doi: 10.1016/ Epub 2011 Oct 3.


Cytochrome P450 (CYP) enzymes are responsible for the metabolism of many exogenous and endogenous compounds. CYPs are abundant in the liver and are also expressed in many extra-hepatic tissues including the brain. Although total CYP levels in the brain are much lower than in the liver, brain CYPs are concentrated near drug targets in specific regions and cell types, and can potentially have a considerable impact on local metabolism. Individual differences in brain CYP metabolism, due to inducers, inhibitors or genetic variation, can influence sensitivity and response to centrally acting drugs. Brain CYPs may also play a role in modulating brain activity, behavior, susceptibility to central nervous system diseases and treatment outcomes. This review highlights recent progress that has been made in understanding the functional significance of CYPs in the brain.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Brain / drug effects
  • Brain / enzymology*
  • Brain / metabolism
  • Cytochrome P-450 Enzyme System / metabolism*
  • Enzyme Induction / drug effects
  • Humans
  • Nerve Tissue Proteins / metabolism*
  • Neurons / drug effects
  • Neurons / enzymology*
  • Neurons / metabolism


  • Nerve Tissue Proteins
  • Cytochrome P-450 Enzyme System