Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1371565 | Bioorganic & Medicinal Chemistry Letters | 2010 | 5 Pages |
Abstract
A backup molecule to compound 2 was sought by targeting the most likely metabolically vulnerable site in this molecule. Compound 18 was subsequently identified as a potent P2X7 antagonist with very low in vivo clearance and high oral bioavailability in all species examined. Some evidence to support the role of P2X7 in the etiology of pain is also presented.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Lee Abberley, Aude Bebius, Paul J. Beswick, Andy Billinton, Katharine L. Collis, David K. Dean, Elena Fonfria, Robert J. Gleave, Stephen J. Medhurst, Anton D. Michel, Andrew P. Moses, Sadhana Patel, Shilina A. Roman, Tiziana Scoccitti, Beverley Smith,