Discovery of N -[(2 S )-5-(6-Fluoro-3-pyridinyl)-2,3-dihydro-1 H -inden-2-yl]-2-propanesulfonamide, a Novel Clinical AMPA Receptor Positive Modulator
2010; American Chemical Society; Volume: 53; Issue: 15 Linguagem: Inglês
10.1021/jm1005429
ISSN1520-4804
AutoresSimon E. Ward, Mark H Harries, Laura Aldegheri, Daniele Andreotti, Stuart P. Ballantine, B.D. Bax, A. I. Harris, A.J. Harker, Jesper Lund, Rosemary A. Melarange, Anna Mingardi, Claudette Mookherjee, J. Mosley, M. Neve, Beatrice Oliosi, Roberto Profeta, Kathrine J. Smith, Paul W. Smith, Simone Spada, Kevin M. Thewlis, Shahnaz P. Yusaf,
Tópico(s)Pharmacological Receptor Mechanisms and Effects
ResumoA 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.
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