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Development of a presynaptic 5-HT 1A antagonist

…, FF Matos, R McGovern, CP VanderMaelen…

文献索引: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 Bioorganic and medicinal chemistry letters, 2003 , vol. 13, # 2 p. 285 - 288

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被引用次数: 17

摘要

A new 5-HT1A silent antagonist 14 (5-HT1A IC50= 2.2 nM) antagonizes the effects of agonists on reciprocal forepaw treading behavior, on neuronal firing in the rat dorsal raphé, and on 5-HT1A release in the raphé 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).