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Pyridyl amides as potent inhibitors of T-type calcium channels |
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| Authors: | Reger Thomas S Yang Zhi-Qiang Schlegel Kelly-Ann S Shu Youheng Mattern Christa Cube Rowena Rittle Kenneth E McGaughey Georgia B Hartman George D Tang Cuyue Ballard Jeanine Kuo Yuhsin Prueksaritanont Thomayant Nuss Cindy E Doran Scott M Fox Steven V Garson Susan L Li Yuxing Kraus Richard L Uebele Victor N Renger John J Barrow James C |
| Institution: | a Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, United States b Department of Drug Metabolism and Pharmacokinetics, Merck Research Laboratories, West Point, PA 19486, United States c Department of Depression and Circadian Disorders, Merck Research Laboratories, West Point, PA 19486, United States |
| Abstract: | A novel series of amide T-type calcium channel antagonists were prepared and evaluated using in vitro and in vivo assays. Optimization of the screening hit 3 led to identification of the potent and selective T-type antagonist 37 that displayed in vivo efficacy in rodent models of epilepsy and sleep. |
| Keywords: | T-type calcium channel Structure-activity relationships Pregnane X receptor Electrocorticogram Epilepsy |
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