ArticleAlcohol (Fayetteville, N.Y.)2012
Positive allosteric modulation of the GABA(B) receptor by GS39783 attenuates the locomotor stimulant actions of ethanol and potentiates the induction of locomotor sensitization.
Article in Alcohol (Fayetteville, N.Y.), 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed, 20 citations in OpenAlex.
- Relationship between GABA-Ergic System and the Expression of Mephedrone-Induced Reward in Rats-Behavioral, Chromatographic and In Vivo Imaging Study.International journal of molecular sciences · 2023Article
- GABAergic signaling in alcohol use disorder and withdrawal: pathological involvement and therapeutic potential.Frontiers in neural circuits · 2023Review
- GABACurrent topics in behavioral neurosciences · 2022Article
- The Novel Positive Allosteric Modulator of the GABAFrontiers in cell and developmental biology · 2021Article
- Ethanol-induced changes in synaptic amino acid neurotransmitter levels in the nucleus accumbens of differentially sensitized mice.Psychopharmacology · 2019Article
- Potential of GABACNS drugs · 2019Review
- A novel cholinergic action of alcohol and the development of tolerance to that effect in Caenorhabditis elegans.Genetics · 2015Article
- Alterations in the rate of binge ethanol consumption: implications for preclinical studies in mice.Addiction biology · 2014Article
- Reversal of morphine analgesic tolerance by ethanol in the mouse.The Journal of pharmacology and experimental therapeutics · 2013Article
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
Acute ethanol-induced locomotor stimulation and ethanol-induced locomotor sensitization are two behavioral assays thought to model the rewarding effects of ethanol. Recent evidence suggests that GS39783, a GABA(B) positive allosteric modulator, may be effective at reducing both the rewarding and reinforcing effects of several drugs of abuse, including ethanol. The goal of this study was to determine if GS39783 was capable of altering acute ethanol-induced stimulation, and the induction and expression of ethanol-induced locomotor sensitization, without effecting basal locomotion levels. Several doses of GS39783 (ranging from 0 to 100 mg/kg, depending on experiment) were tested on adult male DBA/2J mice in four experiments using 3-day basal locomotion and acute ethanol stimulation paradigms, and 14-day induction and expression of ethanol sensitization paradigms. The results of experiment 1 are in agreement with current literature, suggesting that 30 mg/kg doses of GS39783 and lower do not alter basal locomotor activity. In experiment 2, we found that GS39783 significantly decreased acute ethanol stimulation, but only at the 30 mg/kg dose, supporting our hypothesis and other publications suggesting that GABA(B) receptors modulate acute ethanol stimulation. Contrary to our hypothesis, GS39783 did not alter the expression of locomotor sensitization. Additionally, repeated administration of GS39783 in conjunction with ethanol unexpectedly potentiated ethanol-induced locomotor sensitization. Further study of GS39783 is warranted as it may be a more tolerable treatment for alcoholism than full agonists, due to its behavioral efficacy at doses that lack sedative side effects. Our results add to current literature suggesting that the GABA(B) receptor system is indeed involved in the modulation of ethanol-induced locomotor stimulation and sensitization.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.