Progress in GABAA receptor agonists for insomnia disorder

Insomnia is the most common sleep disorder in which an individual has trouble falling or staying asleep. Chronic sleep loss interferes with daily functioning and adversely affects health. The main clinical drugs for insomnia are the positive allosteric modulator of the GABA (gamma-aminobutyric acid)...

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Main Authors: Weiyi Wang (Author), Wanting Fu (Author), Hongyan Zhu (Author), Jing Ma (Author), Jian Zhang (Author), Jia Qi (Author)
Format: Book
Published: Frontiers Media S.A., 2024-11-01T00:00:00Z.
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100 1 0 |a Weiyi Wang  |e author 
700 1 0 |a Wanting Fu  |e author 
700 1 0 |a Hongyan Zhu  |e author 
700 1 0 |a Jing Ma  |e author 
700 1 0 |a Jian Zhang  |e author 
700 1 0 |a Jia Qi  |e author 
245 0 0 |a Progress in GABAA receptor agonists for insomnia disorder 
260 |b Frontiers Media S.A.,   |c 2024-11-01T00:00:00Z. 
500 |a 1663-9812 
500 |a 10.3389/fphar.2024.1432726 
520 |a Insomnia is the most common sleep disorder in which an individual has trouble falling or staying asleep. Chronic sleep loss interferes with daily functioning and adversely affects health. The main clinical drugs for insomnia are the positive allosteric modulator of the GABA (gamma-aminobutyric acid) A receptors (GABAARs) at the benzodiazepine site with selectivity of the GABA-α1 receptor. They are divided into benzodiazepine drugs and non-benzodiazepine drugs. Most recently, the first partial positive allosteric modulator of GABAAR Dimdazenil was approved by National Medical Products Administration (NMPA) and launched in China. This review summarized the mechanism of actions of current clinical drugs for insomnia, and the clinical applications of these drugs, which may help to understand their involvement in insomnia, and to search for more selective and potent ligands to be used in the treatment of insomnia. 
546 |a EN 
690 |a insomnia 
690 |a GABAA receptor 
690 |a benzodiazepines binding site 
690 |a dimdazenil 
690 |a partial positive allosteric modulator 
690 |a Therapeutics. Pharmacology 
690 |a RM1-950 
655 7 |a article  |2 local 
786 0 |n Frontiers in Pharmacology, Vol 15 (2024) 
787 0 |n https://www.frontiersin.org/articles/10.3389/fphar.2024.1432726/full 
787 0 |n https://doaj.org/toc/1663-9812 
856 4 1 |u https://doaj.org/article/93de1b36b3db4b6489ea8afa34cda86c  |z Connect to this object online.