期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 15, 页码 4380-4384出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.05.086
关键词
Histamine; H1; Antihistamine; 2-Aminobenzimidazole; Brain-penetrating; Insomnia
The benzimidazole core of the selective non-brain-penetrating H-1-antihistamine mizolastine was used to identify a series of brain-penetrating H-1-antihistamines for the potential treatment of insomnia. Using cassette PK studies, brain-penetrating H-1-antihistamines were identified and in vivo efficacy was demonstrated in a rat EEG/EMG model. Further optimization focused on strategies to attenuate an identified hERG liability, leading to the discovery of 4i with a promising in vitro pro. le. (C) 2009 Elsevier Ltd. All rights reserved.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据