1050392-36-3Relevant academic research and scientific papers
3-Phenyl-5-isothiazole carboxamides with potent mGluR1 antagonist activity
Fisher, Matthew J.,Backer, Ryan T.,Barth, Vanessa N.,Garbison, Kim E.,Gruber, Joseph M.,Heinz, Beverly A.,Iyengar, Smriti,Hollinshead, Sean P.,Kingston, Anne,Kuklish, Steven L.,Li, Linglin,Nisenbaum, Eric S.,Peters, Steven C.,Phebus, Lee,Simmons, Rosa Maria A.,Van Der Aar, Ellen
, p. 2514 - 2517 (2012/05/05)
The disclosed 3-phenyl-5-isothiazole carboxamides are potent allosteric antagonists of mGluR1 with generally good selectivity relative to the related group 1 receptor mGluR5. Pharmacokinetic properties of a member of this series (1R,2R)-N-(3-(4-methoxyphenyl)-4-methylisothiazol-5-yl)-2- methylcyclopropanecarboxamide (14) are good, showing acceptable plasma and brain exposure after oral dosing. Oral administration of isothiazole 14 gave robust activity in the formalin model of persistent pain which correlated with CNS receptor occupancy.
SUBSTITUTED CARBOXAMIDES
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, (2008/12/08)
This application relates to a substituted carboxamide compound of formula I, or a pharmaceutically acceptable salt thereof, as defined herein, a pharmaceutical composition thereof, and its use in treating pain.
