Positive allosteric modulators of the GABAB receptor: a new class of ligands with therapeutic potential for alcohol use disorder.
Alcohol Alcohol
; 59(3)2024 Mar 16.
Article
en En
| MEDLINE
| ID: mdl-38566580
ABSTRACT
BACKGROUND:
Positive allosteric modulators (PAMs) of the GABAB receptor constitute a new class of GABAB-receptor ligands. GABAB PAMs reproduce several pharmacological effects of the orthosteric GABAB receptor agonist, baclofen, although displaying a better safety profile.AIMS:
This paper reviews the reducing or, frequently, even suppressing effects of all GABAB PAMs tested to date on multiple alcohol-related behaviours in laboratory rodents exposed to validated experimental models of human alcohol use disorder.RESULTS:
Acute or repeated treatment with CGP7930, GS39783, BHF177, rac-BHFF, ADX71441, CMPPE, COR659, ASP8062, KK-92A, and ORM-27669 reduced excessive alcohol drinking, relapse- and binge-like drinking, operant alcohol self-administration, reinstatement of alcohol seeking, and alcohol-induced conditioned place preference in rats and mice.CONCLUSIONS:
These effects closely mirrored those of baclofen; notably, they were associated to remarkably lower levels of tolerance and toxicity. The recent transition of ASP8062 to clinical testing will soon prove whether these highly consistent preclinical data translate to AUD patients.Palabras clave
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Base de datos:
MEDLINE
Asunto principal:
Alcoholismo
Límite:
Animals
Idioma:
En
Revista:
Alcohol Alcohol
Año:
2024
Tipo del documento:
Article
País de afiliación:
Italia