GABAB receptor ligands for the treatment of alcohol use disorder: preclinical and clinical evidence
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-induce...
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| Format: | Article |
| Language: | English |
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Frontiers Media S.A.
2014-06-01
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| Series: | Frontiers in Neuroscience |
| Subjects: | |
| Online Access: | http://journal.frontiersin.org/Journal/10.3389/fnins.2014.00140/full |
| _version_ | 1828748953485574144 |
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| author | Roberta eAgabio Giancarlo eColombo |
| author_facet | Roberta eAgabio Giancarlo eColombo |
| author_sort | Roberta eAgabio |
| collection | DOAJ |
| description | 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). |
| first_indexed | 2024-12-10T11:44:25Z |
| format | Article |
| id | doaj.art-5a3d867ca1bb4164af8553d75b555384 |
| institution | Directory Open Access Journal |
| issn | 1662-453X |
| language | English |
| last_indexed | 2024-12-10T11:44:25Z |
| publishDate | 2014-06-01 |
| publisher | Frontiers Media S.A. |
| record_format | Article |
| series | Frontiers in Neuroscience |
| spelling | doaj.art-5a3d867ca1bb4164af8553d75b5553842022-12-22T01:50:09ZengFrontiers Media S.A.Frontiers in Neuroscience1662-453X2014-06-01810.3389/fnins.2014.0014091835GABAB receptor ligands for the treatment of alcohol use disorder: preclinical and clinical evidenceRoberta eAgabio0Giancarlo eColombo1University of CagliariNational Research Council of ItalyThe 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).http://journal.frontiersin.org/Journal/10.3389/fnins.2014.00140/fullBaclofenGABAB receptoralcohol use disorderPositive allosteric modulatorsAnimal models of alcohol use disorder |
| spellingShingle | Roberta eAgabio Giancarlo eColombo GABAB receptor ligands for the treatment of alcohol use disorder: preclinical and clinical evidence Frontiers in Neuroscience Baclofen GABAB receptor alcohol use disorder Positive allosteric modulators Animal models of alcohol use disorder |
| title | GABAB receptor ligands for the treatment of alcohol use disorder: preclinical and clinical evidence |
| title_full | GABAB receptor ligands for the treatment of alcohol use disorder: preclinical and clinical evidence |
| title_fullStr | GABAB receptor ligands for the treatment of alcohol use disorder: preclinical and clinical evidence |
| title_full_unstemmed | GABAB receptor ligands for the treatment of alcohol use disorder: preclinical and clinical evidence |
| title_short | GABAB receptor ligands for the treatment of alcohol use disorder: preclinical and clinical evidence |
| title_sort | gabab receptor ligands for the treatment of alcohol use disorder preclinical and clinical evidence |
| topic | Baclofen GABAB receptor alcohol use disorder Positive allosteric modulators Animal models of alcohol use disorder |
| url | http://journal.frontiersin.org/Journal/10.3389/fnins.2014.00140/full |
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