Dopamine D3 receptor antagonists as therapeutic agents

Drug Discov Today. 2005 Jul 1;10(13):917-25. doi: 10.1016/S1359-6446(05)03491-4.


The behavioral and pathophysiological role of the dopamine D(3) receptor, which was deduced from anatomical, lesion and drug treatment studies in the ten years following cloning of the receptor, indicated that its functions differed from those of the D(2) receptor. There is increasingly strong evidence that D(3) receptor antagonists will be effective antipsychotic agents. In this regard, an amelioration of the negative and cognitive symptoms of schizophrenia holds the most promise for D(3) receptor antagonists, a concept currently under clinical evaluation. In addition, D(3) receptors could be involved in behavioral sensitization and the potential application of D(3) receptor antagonists in the treatment of drug abuse is undergoing intensive experimental investigation.

Publication types

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

MeSH terms

  • Animals
  • Dopamine Antagonists / chemistry
  • Dopamine Antagonists / therapeutic use*
  • Humans
  • Molecular Structure
  • Nitriles / therapeutic use
  • Receptors, Dopamine D3 / antagonists & inhibitors*
  • Receptors, Dopamine D3 / physiology
  • Substance-Related Disorders / physiopathology
  • Substance-Related Disorders / prevention & control
  • Technology, Pharmaceutical / methods
  • Technology, Pharmaceutical / trends
  • Tetrahydroisoquinolines / therapeutic use


  • Dopamine Antagonists
  • Nitriles
  • Receptors, Dopamine D3
  • SB 277011
  • Tetrahydroisoquinolines