Targeting GABAB receptors for anti-Abuse drug discovery

Tamara J. Phillips, Cheryl Reed

Research output: Contribution to journalReview articlepeer-review

25 Scopus citations


Introduction: There is increasing evidence encouraging the development of drugs that positively modulate the γ-Aminobutyric acid type B (GABAB) receptor for combating addiction. Compounds that target GABAB receptors are unique as anti-Abuse therapies because of their impact against multiple addictive drugs.Areas covered: The authors present the basic information concerning the drug actions of GABA and GABAB receptor orthosteric agonists and positive allosteric modulators (PAM). Furthermore, they discuss several recent excellent reviews and newer results pertaining to GABAB receptor drug effects on responses to and self-Administration of: alcohol (ethanol), nicotine, cocaine, (meth)amphetamine, and opioids. Preclinical and clinical data are considered.Expert opinion: Clinical data exist only for baclofen and mostly for alcohol use disorders. Additional trials are needed, but effects are promising. Whether PAMs, given alone or in combination with a direct GABAB receptor agonist, will be clinically effective and have fewer side effects requires investigation. The sedative effects of baclofen, a Food and Drug Administration (FDA)-Approved drug, become less severe over time. Based on existing data, baclofen is well-tolerated. However, genetic and physiological differences are likely to contribute to individual responses to different therapeutic agents. The more immediate development of baclofen as a therapeutic for alcohol use disorders may be of significant benefit to some individuals.

Original languageEnglish (US)
Pages (from-to)1307-1317
Number of pages11
JournalExpert Opinion on Drug Discovery
Issue number11
StatePublished - Nov 1 2014


  • Addiction
  • Alcohol
  • Amphetamine
  • Baclofen
  • Cocaine
  • Ethanol
  • Methamphetamine
  • Nicotine
  • Opioid
  • Positive allosteric modulator

ASJC Scopus subject areas

  • Drug Discovery


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