Highly potent, non-basic 5-HT6 ligands. Site mutagenesis evidence for a second binding mode at 5-HT6 for antagonism
Highly potent, non-basic 5-HT6 ligands. Site mutagenesis evidence for a second binding mode at 5-HT6 for antagonism
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DOI：
10.1016/j.bmcl.2010.03.110
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发表时间：
2010-06-01
影响因子：
2.7
通讯作者：
Mirzadegan, Tara
中科院分区：
文献类型：
--
作者：
Harris, Ralph N., III;Stabler, Russel S.;Mirzadegan, Tara
制备了一系列衍生自（R）-1-（氨基）甲基-6-（苯基）磺酰基四氢化萘的5-HT 6配体，其产生了几种具有亚纳摩尔亲和力的非碱性类似物。配体结构-活性关系、受体点突变研究和这些新型配体的分子建模都结合起来揭示了5-HT 6拮抗作用的新的替代结合模式。(C)2010年由Elsevier Ltd.出版
A series of 5-HT6 ligands derived from (R)-1-(amino) methyl-6-(phenyl) sulfonyltetralin was prepared that yielded several non-basic analogs having sub-nanomolar affinity. Ligand structure-activity relationships, receptor point mutation studies, and molecular modeling of these novel ligands all combined to reveal a new alternative binding mode to 5-HT6 for antagonism. (C) 2010 Published by Elsevier Ltd.