PMID: 22574677May 12, 2012Paper

The development of medications for alcohol-use disorders targeting the GABAB receptor system

Recent Patents on CNS Drug Discovery
Roberta AgabioGiancarlo Colombo

Abstract

The present paper summarizes experimental and clinical data suggesting the therapeutic potential of the prototypic GABAB receptor agonist, baclofen, for the treatment of alcohol-use disorders (AUDs). Numerous studies have reported baclofen-induced suppression of alcohol drinking, relapse-like drinking, and alcohol reinforcing, rewarding, stimulating, and motivational properties in rats and mice. The majority of clinical surveys conducted to date have demonstrated the capacity of baclofen to suppress alcohol consumption, craving for alcohol, and alcohol withdrawal symptomatology in alcohol-dependent patients. More recently, the discovery of a positive allosteric modulatory binding site, together with the synthesis of in vivo effective ligands, provided a new tool for pharmacological manipulations of the GABAB receptor. Accumulating lines of preclinical evidence suggest that positive allosteric modulators of the GABAB receptor (GABAB PAMs), such as GS39783, display a high therapeutic index and retain baclofen's capacity to suppress alcohol consumption and alcohol reinforcing and motivational properties. The present paper also summarizes the most relevant patents on GABAB receptor agonists and GABAB PAMs as possible pharmacotherap...Continue Reading

Citations

Jan 1, 2013·The Journal of Pharmacology and Experimental Therapeutics·Wouter KoekKenner C Rice
Sep 10, 2014·Expert Opinion on Drug Discovery·Tamara J Phillips, Cheryl Reed
Nov 20, 2015·Progress in Neuro-psychopharmacology & Biological Psychiatry·C E Van SkikeK Nixon
Aug 19, 2015·Neuroscience and Biobehavioral Reviews·Chelsea R Kasten, Stephen L Boehm
Jul 13, 2014·European Journal of Pharmacology·Amir H Rezvani, Edward D Levin
Jun 19, 2013·European Addiction Research·Roberta AgabioGian Luigi Gessa
Mar 27, 2013·The Journal of Pharmacology and Experimental Therapeutics·L C HullW L Dewey
Jan 11, 2020·Neurotherapeutics : the Journal of the American Society for Experimental NeuroTherapeutics·Jérémie NeastaSami Ben Hamida

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