Short-acting T-type calcium channel antagonists significantly modify sleep architecture in rodents

…, J Small, GD Hartman, J Ballard, C Tang…

文献索引：Yang, Zhi-Qiang; Schlegel, Kelly-Ann S.; Shu, Youheng; Reger, Thomas S.; Cube, Rowena; Mattern, Christa; Coleman, Paul J.; Small, Jim; Hartman, George D.; Ballard, Jeanine; Tang, Cuyue; Kuo, Yuhsin; Prueksaritanont, Thomayant; Nuss, Cindy E.; Doran, Scott; Fox, Steve V.; Garson, Susan L.; Li, Yuxing; Kraus, Richard L.; Uebele, Victor N.; Taylor, Adekemi B.; Zeng, Wei; Fang, Wei; Chavez-Eng, Cynthia; Troyer, Matthew D.; Luk, Julie Ann; Laethem, Tine; Cook, William O.; Renger, John J.; Barrow, James C. ACS Medicinal Chemistry Letters, 2010 , vol. 1, # 9 p. 504 - 509

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被引用次数: 7

摘要

A novel phenyl acetamide series of short-acting T-type calcium channel antagonists has been identified and evaluated using in vitro and in vivo assays. Heterocycle substitutions of the 4-position of the phenyl acetamides afforded potent and selective antagonists that exhibited desired short plasma half-lives across preclinical species. Lead compound TTA- A8 emerged as a compound with excellent in vivo efficacy as indicated by its significant ...