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Effect of modifications of the alkylpiperazine moiety of trazodone on 5HT2A and α1 receptor binding affinity

M Giannangeli, N Cazzolla, MR Luparini…

文献索引:Giannangeli, Marilena; Cazzolla, Nicola; Luparini, Maria Rita; Magnani, Maurizio; Mabilia, Massimo; Picconi, Giuseppe; Tomaselli, Mauro; Baiocchi, Leandro Journal of Medicinal Chemistry, 1999 , vol. 42, # 3 p. 336 - 345

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被引用次数: 31

摘要

A series of triazolopyridine derivatives (compounds 2a-l) were synthesized in order to explore the effect of modifications of the alkylpiperazine moiety of trazodone (fragment A) on binding affinity for 5HT2A and α1 receptors. All of the synthesized compounds show a decrease of affinity for both 5HT2A and α1 receptors, as compared to trazodone, with the exception of compounds 2b, c which bear a methyl group in an α position to the aliphatic ...