150019-57-1Relevant articles and documents
CHEMOKING RECEPTOR ANTAGONISTS
-
Page/Page column 220, (2013/03/26)
Disclosed herein are chemokine receptor antagonists of formula (I) wherein G1, X1, X2, and X3 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.
Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2
Xue, Chu-Biao,Wang, Anlai,Meloni, David,Zhang, Ke,Kong, Ling,Feng, Hao,Glenn, Joseph,Huang, Taisheng,Zhang, Yingxin,Cao, Ganfeng,Anand, Rajan,Zheng, Changsheng,Xia, Michael,Han, Qi,Robinson,Storace, Lou,Shao, Lixin,Li, Mei,Brodmerkel, Carrie M.,Covington, Maryanne,Scherle, Peggy,Diamond, Sharon,Yeleswaram, Swamy,Vaddi, Kris,Newton, Robert,Hollis, Greg,Friedman, Steven,Metcalf, Brian
experimental part, p. 7473 - 7478 (2011/01/12)
Rational design based on a pharmacophore of CCR2 antagonists reported in the literature identified lead compound 9a with potent inhibitory activity against human CCR2 (hCCR2) but moderate activity against murine CCR2 (mCCR2). Modification on 9a led to the
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).