| Literature DB >> 18540666 |
William D Shipe1, James C Barrow, Zhi-Qiang Yang, Craig W Lindsley, F Vivien Yang, Kelly-Ann S Schlegel, Youheng Shu, Kenneth E Rittle, Mark G Bock, George D Hartman, Cuyue Tang, Jeanine E Ballard, Yuhsin Kuo, Emily D Adarayan, Thomayant Prueksaritanont, Matthew M Zrada, Victor N Uebele, Cindy E Nuss, Thomas M Connolly, Scott M Doran, Steven V Fox, Richard L Kraus, Michael J Marino, Valerie Kuzmick Graufelds, Hugo M Vargas, Patricia B Bunting, Martha Hasbun-Manning, Rose M Evans, Kenneth S Koblan, John J Renger.
Abstract
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.Entities:
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Year: 2008 PMID： 18540666 DOI： 10.1021/jm800419w
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446