40503-85-3Relevant articles and documents
Overcoming hERG activity in the discovery of a series of 4-azetidinyl-1-aryl-cyclohexanes as CCR2 antagonists
Zhang, Xuqing,Hufnagel, Heather,Markotan, Thomas,Lanter, James,Cai, Chaozhong,Hou, Cuifen,Singer, Monica,Opas, Evan,McKenney, Sandra,Crysler, Carl,Johnson, Dana,Sui, Zhihua
supporting information; experimental part, p. 5577 - 5582 (2011/10/09)
A series of 4-azetidinyl-1-aryl-cyclohexanes as potent CCR2 antagonists with high selectivity over activity for the hERG potassium channel is discovered through divergent SARs of CCR2 and hERG.
Development of a presynaptic 5-HT1A antagonist.
Mattson, Ronald J,Catt, John D,Sloan, Charles P,Gao,Carter, Richard B,Gentile, Anthony,Mahle, Cathy D,Matos, F Fatima,McGovern, Rachel,VanderMaelen, Cam P,Yocca, Frank D
, p. 285 - 288 (2007/10/03)
A new 5-HT(1A) silent antagonist 14 (5-HT(1A) IC(50)=2.2 nM) antagonizes the effects of agonists on reciprocal forepaw treading behavior, on neuronal firing in the rat dorsal raphe, and on 5-HT(1A) release in the raphe and hippocampus. While 14 alone was inactive in the social interaction paradigm, it completely reversed the social interaction activity of the serotonergic compounds (buspirone, 1, and 2).