3-Phenyl-5-isothiazole carboxamides with potent mGluR1 antagonist activity.

Matthew J Fisher,Ryan T Backer,Vanessa N Barth,Kim E Garbison,Joseph M Gruber,Beverly A Heinz,Smriti Iyengar,Sean P Hollinshead,Anne Kingston,Steven L Kuklish,Linglin Li,Eric S Nisenbaum,Steven C Peters,Lee Phebus,Rosa Maria A Simmons,Ellen van der Aar

Bioorganic & Medicinal Chemistry Letters（2012）

引用 23|浏览19

暂无评分

摘要

The disclosed 3-phenyl-5-isothiazole carboxamides are potent allosteric antagonists of mGluR1. Oral administration of one member of this series (1R,2R)-N-(3-(4-methoxyphenyl)-4-methylisothiazol-5-yl)-2-methylcyclopropanecarboxamide (14) afforded both dose responsive CNS mGlu1 receptor occupancy and correlative efficacy in the formalin model of persistent pain.

查看译文

关键词

mGluR1,Receptor occupancy,Formalin model

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