150019-57-1Relevant articles and documents
CHEMOKING RECEPTOR ANTAGONISTS
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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.
4-AZETIDINYL-1-PHENYL-CYCLOHEXANE ANTAGONISTS OF CCR2
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Page/Page column 44, (2010/11/03)
The present invention comprises compounds of Formula (I): wherein: X, R1, R2, R3, and R4 are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
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).