| Literature DB >> 20934331 |
Lee Abberley1, 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, Jon G A Steadman, Daryl S Walter.
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 P2X(7) antagonist with very low in vivo clearance and high oral bioavailability in all species examined. Some evidence to support the role of P2X(7) in the etiology of pain is also presented.Entities:
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Year: 2010 PMID： 20934331 DOI： 10.1016/j.bmcl.2010.09.101
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823