新型选择性σ1配体的设计、合成及构效关系分析
Design, synthesis, and SAR analysis of novel selective sigma1 ligands.
作者信息
Collina Simona, Loddo Guya, Urbano Mariangela, Linati Laura, Callegari Athos, Ortuso Francesco, Alcaro Stefano, Laggner Christian, Langer Thierry, Prezzavento Orazio, Ronsisvalle Giuseppe, Azzolina Ornella
机构信息
Dipartimento di Chimica Farmaceutica, Università di Pavia, Viale Taramelli 12, 27100 Pavia, Italy.
出版信息
Bioorg Med Chem. 2007 Jan 15;15(2):771-83. doi: 10.1016/j.bmc.2006.10.048. Epub 2006 Oct 25.
A new series of arylalkyl- and alkenylamines was designed, synthesized, and evaluated for binding to sigma(1) and sigma(2) receptors. Many compounds exhibited nanomolar affinity for sigma(1) subtype receptor with good selectivity over sigma(2). A molecular modeling study was conducted in order to rationalize the experimental data, and the structure-receptor affinities are discussed.
设计、合成并评估了一系列新型芳基烷基胺和烯基胺与σ(1)和σ(2)受体的结合情况。许多化合物对σ(1)亚型受体表现出纳摩尔亲和力，对σ(2)具有良好的选择性。进行了分子模拟研究以合理解释实验数据，并讨论了结构与受体的亲和力。
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