Dienstag 16. September 2014, 23:56
@all,
bezüglich Baclofen / GABA-B-Agonisten sehr optimistischer Übersichtsartikel :
GABAB receptor ligands for the treatment of alcohol use disorder: preclinical and clinical evidence(pdf kann in Vollversion runtergeladen werden -oben rechts-)
REVIEW ARTICLE Front. Neurosci., 06 June 2014 | doi: 10.3389/fnins.2014.00140
Roberta Agabio1 and Giancarlo Colombo2*
1Department of Biomedical Sciences, University of Cagliari, Monserrato, Italy
2Section of Cagliari, Neuroscience Institute, National Research Council of Italy, Monserrato, Italy
Auszug:
"The present paper summarizes the preclinical and clinical studies conducted to define the “anti-alcohol” pharmacological profile of the prototypic GABAB receptor agonist, baclofen, and its therapeutic potential for treatment of alcohol use disorder (AUD). Numerous studies have reported baclofen-induced suppression of alcohol drinking (including relapse- and binge-like drinking) and alcohol reinforcing, motivational, stimulating, and rewarding properties in rodents and monkeys. The majority of clinical surveys conducted to date—including case reports, retrospective chart reviews, and randomized placebo-controlled studies—suggest the ability of baclofen to suppress alcohol consumption, craving for alcohol, and alcohol withdrawal symptomatology in alcohol-dependent patients. The recent identification of a positive allosteric modulatory binding site, together with the synthesis of in vivo effective ligands, represents a novel, and likely more favorable, option for pharmacological manipulations of the GABAB receptor. Accordingly, data collected to date suggest that positive allosteric modulators of the GABAB receptor reproduce several “anti-alcohol” effects of baclofen and display a higher therapeutic index (with larger separation—in terms of doses—between “anti-alcohol” effects and sedation)."
Kurzfassung auf deutsch :
"Durch eine allosterische Modifikation des GABA-B-Rezeptors können vielleicht Substanzen gefunden werden, die wie Baclofen wirken aber weniger Nebenwirkungen (z.B. Sedierung) bewirken."
Also : Das Konzept der GABA-B-Agonisten kann/sollte weiterentwickelt werden...
LG, Werner