Zhu Wenwen, Huang Lishan, Cheng Hanxing, Li Nanxi, Zhang Bin, Dai Wenbin, Wu Xiao, Zhang Dechou, Feng Wenzhan, Li Sen, Xu Houping
Geriatric Department, The Affiliated Traditional Chinese Medicine Hospital, Southwest Medical University, Luzhou, Sichuan, China.
College of Integrative Medicine, The Affiliated Traditional Chinese Medicine Hospital, Southwest Medical University, Luzhou, Sichuan, China.
Heliyon. 2024 Nov 23;10(23):e40665. doi: 10.1016/j.heliyon.2024.e40665. eCollection 2024 Dec 15.
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.
失眠现已成为一个全球关注的主要健康问题,约有三分之一的人口存在睡眠问题,且这一比例仍在逐年上升。目前临床实践中使用的大多数失眠治疗药物并非靶向研发,而是偶然发现的,并且存在成瘾等不可避免的副作用。寻找更安全、更有效的治疗药物已成为当前研究的迫切需求。γ-氨基丁酸(GABA)是中枢神经系统中的主要抑制性神经递质。它可以改善失眠、阿尔茨海默病、帕金森病、癫痫和其他神经系统疾病。已有多种机制被报道与GABA改善失眠有关,如GABAA受体调节、GABAB受体调节、抑制神经炎症反应、修复氧化损伤以及昼夜节律激素褪黑素的相互调节。GABA是预防和治疗失眠的潜在治疗靶点。本文综述了GABA及其受体在失眠疾病中的作用机制以及GABA类似物应用的潜力,并讨论了GABA作为一种有前景的失眠治疗药物的研究进展。这将有助于新型靶向GABA类药物的开发,并为失眠的临床治疗提供新的思路和方法。