Regulators of G protein signaling & drugs of abuse

Mol Interv. 2005 Feb;5(1):30-41. doi: 10.1124/mi.5.1.7.


Drugs of abuse such as opioids and stimulants share a common dopaminergic reward pathway; however, in response to continual intermittent exposure to such drugs, there are neuronal alterations leading to changes in behavior. Regulators of G protein signaling (RGS) are proteins that negatively regulate G protein signaling and are expressed in brain areas important for the pharmacology of abused drugs. Moreover, the level of expression of several of these proteins is regulated by abused drugs. In this article, we discuss RGS proteins, their regulation by morphine and stimulants, and how altered levels of these proteins affect cell signaling to contribute to the pharmacology and behavioral consequence of abused drugs. Finally, we consider if RGS proteins represent viable targets for drug abuse medications.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • Animals
  • Humans
  • Illicit Drugs / metabolism
  • Illicit Drugs / pharmacology*
  • Mutant Proteins / metabolism
  • Nervous System / drug effects
  • Nervous System / metabolism
  • RGS Proteins / metabolism*
  • Signal Transduction / drug effects*
  • Substance-Related Disorders / therapy


  • Illicit Drugs
  • Mutant Proteins
  • RGS Proteins