Identification of 2-oxo-N-(phenylmethyl)-4-imidazolidinecarboxamide antagonists of the P2X7 receptor

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,Jon G.A. Steadman,Daryl S. Walter

Bioorganic & Medicinal Chemistry Letters（2010）

引用 31|浏览45

暂无评分

摘要

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.

查看译文

关键词

P2X7,Antagonist,Pain

AI 理解论文

溯源树

样例

生成溯源树，研究论文发展脉络

Chat Paper

正在生成论文摘要