Teegarden Bradley R, Al Shamma Hussien, Xiong Yifeng
Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, CA 92121, USA.
Curr Top Med Chem. 2008;8(11):969-76. doi: 10.2174/156802608784936700.
Nearly one half of the adult population in the U.S. experience some symptoms of insomnia (difficulties with getting to sleep, maintaining sleep, and/or sleep quality) on a weekly basis. Although most people with insomnia complain primarily of issues related to sleep maintenance and quality, current therapeutic approaches, including GABA(A) agonists, off label antidepressant use, H(1) antagonists and melatonin agonists, primarily address sleep onset latency. The overall sleep architecture, especially that of the deeper stages of NREM sleep known as slow wave sleep (SWS), plays a crucial role in restorative, restful sleep. Through the 5-HT(2A) receptor, serotonin plays an active role in the regulation of sleep architecture. Antagonists / inverse-agonists of 5-HT(2A), such as APD125, volinanserin, eplivanserin, pruvanserin and pimavanserin, are currently being investigated as therapeutics that could improve the treatment of sleep maintenance and quality in people with insomnia.
美国近一半的成年人每周都会出现一些失眠症状（入睡困难、维持睡眠困难和/或睡眠质量差）。尽管大多数失眠患者主要抱怨与睡眠维持和质量相关的问题，但目前的治疗方法，包括GABA(A)激动剂、非标签使用抗抑郁药、H(1)拮抗剂和褪黑素激动剂，主要针对的是入睡潜伏期。整体睡眠结构，尤其是被称为慢波睡眠（SWS）的非快速眼动睡眠更深阶段的结构，在恢复性、安宁的睡眠中起着至关重要的作用。血清素通过5-HT(2A)受体在睡眠结构的调节中发挥积极作用。5-HT(2A)的拮抗剂/反向激动剂，如APD125、沃利色林、依普利色林、普鲁万色林和匹莫万色林，目前正在作为可能改善失眠患者睡眠维持和质量治疗的药物进行研究。
