期刊
CHEMMEDCHEM
卷 9, 期 11, 页码 2486-2496出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.201402258
关键词
insomnia; neurotransmitters; orexin receptor antagonists; peptides; stress-related disorders
The orexin system consists of two G-protein-coupled receptors, the orexin1 and orexin2 receptors, widely expressed in diverse regions of the brain, and two peptide agonists, orexinA and orexinB, which are produced in a small assembly of neurons in the lateral hypothalamus. The orexin system plays an important role in the maintenance of wakefulness. Several compounds (almorexant, SB-649868, suvorexant) have been in advanced clinical trials for treating primary insomnia. ACT-462206 is a new, potent, and selective dual orexin receptor antagonist (DORA) that inhibits the stimulating effects of the orexin peptides at both the orexin1 and 2 receptors. It decreases wakefulness and increases non-rapid eye movement (non-REM) and REM sleep while maintaining natural sleep architectures in rat and dog electroencephalography/electromyography (EEG/EMG) experiments. ACT-462206 shows anxiolytic-like properties in rats without affecting cognition and motor function. It is therefore a potential candidate for the treatment of insomnia.
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