Shipe William D, Barrow James C, Yang Zhi-Qiang, Lindsley Craig W, Yang F Vivien, Schlegel Kelly-Ann S, Shu Youheng, Rittle Kenneth E, Bock Mark G, Hartman George D, Tang Cuyue, Ballard Jeanine E, Kuo Yuhsin, Adarayan Emily D, Prueksaritanont Thomayant, Zrada Matthew M, Uebele Victor N, Nuss Cindy E, Connolly Thomas M, Doran Scott M, Fox Steven V, Kraus Richard L, Marino Michael J, Graufelds Valerie Kuzmick, Vargas Hugo M, Bunting Patricia B, Hasbun-Manning Martha, Evans Rose M, Koblan Kenneth S, Renger John J
Department of Medicinal Chemistry, Merck Research Laboratories, WP14-1, P.O. Box 4, Sumneytown Pike, West Point, Pennsylvania 19486, USA.
J Med Chem. 2008 Jul 10;51(13):3692-5. doi: 10.1021/jm800419w. Epub 2008 Jun 10.
The novel T-type antagonist ( S)- 5 has been prepared and evaluated in in vitro and in vivo assays for T-type calcium ion channel activity. Structural modification of the piperidine leads 1 and 2 afforded the fluorinated piperidine ( S)- 5, a potent and selective antagonist that displayed in vivo CNS efficacy without adverse cardiovascular effects.
新型T型拮抗剂（S）-5已被制备，并在体外和体内进行了T型钙离子通道活性测定。对哌啶前体1和2进行结构修饰得到了氟化哌啶（S）-5，它是一种强效且选择性的拮抗剂，在体内显示出中枢神经系统疗效且无不良心血管影响。
