| Literature DB >> 20614889 |
Simon E Ward1, Mark Harries, Laura Aldegheri, Daniele Andreotti, Stuart Ballantine, Benjamin D Bax, Andrew J Harris, Andy J Harker, Jesper Lund, Rosemary Melarange, Anna Mingardi, Claudette Mookherjee, Julie Mosley, Marta Neve, Beatrice Oliosi, Roberto Profeta, Kathrine J Smith, Paul W Smith, Simone Spada, Kevin M Thewlis, Shahnaz P Yusaf.
Abstract
A series of AMPA receptor positive allosteric modulators has been optimized from poorly penetrant leads to identify molecules with excellent preclinical pharmacokinetics and CNS penetration. These discoveries led to 17i, a potent, efficacious CNS penetrant molecule with an excellent pharmacokinetic profile across preclinical species, which is well tolerated and is also orally bioavailable in humans.Entities:
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Year: 2010 PMID： 20614889 DOI： 10.1021/jm1005429
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446