Fatty acid amide hydrolase: an emerging therapeutic target in the endocannabinoid system

Curr Opin Chem Biol. 2003 Aug;7(4):469-75. doi: 10.1016/s1367-5931(03)00079-6.


The medicinal properties of exogenous cannabinoids have been recognized for centuries and can largely be attributed to the activation in the nervous system of a single G-protein-coupled receptor, CB1. However, the beneficial properties of cannabinoids, which include relief of pain and spasticity, are counterbalanced by adverse effects such as cognitive and motor dysfunction. The recent discoveries of anandamide, a natural lipid ligand for CB1, and an enzyme, fatty acid amide hydrolase (FAAH), that terminates anandamide signaling have inspired pharmacological strategies to augment endogenous cannabinoid ('endocannabinoid') activity with FAAH inhibitors, which might exhibit superior selectivity in their elicited behavioral effects compared with direct CB1 agonists.

Publication types

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

MeSH terms

  • Amidohydrolases / antagonists & inhibitors
  • Amidohydrolases / genetics
  • Amidohydrolases / metabolism*
  • Animals
  • Arachidonic Acids / metabolism
  • Cannabinoid Receptor Modulators / metabolism*
  • Cannabinoids / antagonists & inhibitors
  • Cannabinoids / metabolism
  • Crystallography, X-Ray
  • Drug Delivery Systems
  • Drug Design
  • Endocannabinoids*
  • Enzyme Inhibitors / therapeutic use*
  • Humans
  • Molecular Structure
  • Polyunsaturated Alkamides
  • Receptor, Cannabinoid, CB1 / metabolism


  • Arachidonic Acids
  • Cannabinoid Receptor Modulators
  • Cannabinoids
  • Endocannabinoids
  • Enzyme Inhibitors
  • Polyunsaturated Alkamides
  • Receptor, Cannabinoid, CB1
  • Amidohydrolases
  • fatty-acid amide hydrolase
  • anandamide