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Review
. 2024 Nov 23;10(23):e40665.
doi: 10.1016/j.heliyon.2024.e40665. eCollection 2024 Dec 15.

GABA and its receptors' mechanisms in the treatment of insomnia

Wenwen Zhu  1 , Lishan Huang  1 , Hanxing Cheng  1 , Nanxi Li  1 , Bin Zhang  1 , Wenbin Dai  1 , Xiao Wu  2 , Dechou Zhang  2 , Wenzhan Feng  2 , Sen Li  3 , Houping Xu  1
Affiliations
Review

GABA and its receptors' mechanisms in the treatment of insomnia

Wenwen Zhu et al. Heliyon. .

Abstract

Insomnia has now become a major health problem of global concern, with about 1/3 of the population suffering from sleep problems, a proportion that is still rising year by year. Most of the therapeutic drugs for insomnia currently used in clinical practice are not developed in a targeted manner, but are discovered by chance, and have unavoidable side effects such as addiction. Finding a safer and more effective therapeutic drug has become an urgent need for current research. Gamma-aminobutyric acid (GABA) is the major inhibitory neurotransmitter in the central nervous system. It can ameliorate Insomnia, Alzheimer's disease, Parkinson's disease, Epilepsy, and other neurological disorders. Various mechanisms have been reported for GABA to ameliorate insomnia, such as GABAA receptor modulation, GABAB receptor modulation, inhibition of neuroinflammatory responses, repair of oxidative damage, and inter-regulation of the circadian rhythm hormone melatonin. GABA is a potential therapeutic target in the prevention and treatment of insomnia. This paper reviews mechanisms of GABA and its receptors in insomnia diseases and the potential of GABA analogs application and discusses the research progress of GABA as a promising therapeutic drug for insomnia diseases. This will help the development of novel targeted GABA-like drugs and provide new ideas and methods for the clinical treatment of insomnia.

Keywords: GABA; Insomnia; Mechanisms; Neuroinflammation.

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Conflict of interest statement

The authors declare the following financial interests/personal relationships which may be considered as potential competing interests:Houping Xu reports financial support was provided by 10.13039/501100014895Southwest Medical University Technology Program. Houping Xu reports financial support was provided by Peng Zhou People's Hospital-10.13039/501100014895Southwest Medical University 10.13039/100019767Cooperation Program. Houping Xu reports financial support was provided by People's Government of Luzhou City-10.13039/501100014895Southwest Medical University Science and Technology Strategic 10.13039/100019767Cooperation Project. Houping Xu reports financial support was provided by 10.13039/501100016350Administration of Traditional Chinese Medicine of Sichuan Province. Xiao Wu reports financial support was provided by 10.13039/501100016350Administration of Traditional Chinese Medicine of Sichuan Province. Xiao Wu reports financial support was provided by Sichuan Science and Technology Department Project. If there are other authors, they declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

Figures

Fig. 1
Fig. 1
GABA and its receptors in insomnia.
Fig. 2
Fig. 2
Structure, binding site and mechanism of action of GABAA receptors.
Fig. 3
Fig. 3
Structure, binding site and mechanism of action of GABAB receptors.
Fig. 4
Fig. 4
Mechanisms of GABA inhibition of inflammation in macrophages.
Fig. 5
Fig. 5
Mechanisms of GABA inhibition of inflammation in microglia.
Fig. 6
Fig. 6
Mechanism of mutual regulation of GABA and melatonin.
See this image and copyright information in PMC

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