1,2,3,4-tetrahydrocarbazoles as 5-HT6 serotonin receptor ligands.
1,2,3,4-tetrahydrocarbazoles as 5-HT6 serotonin receptor ligands.
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1,2,3,4-四氢咔唑作为 5-HT6 血清素受体配体。
DOI：
10.1016/j.bmcl.2004.01.071
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发表时间：
2004
期刊：
影响因子：
--
通讯作者：
Glennon,RichardA
中科院分区：
文献类型：
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作者：
Chang-Fong,Jean;Rangisetty,JagadeeshB;Dukat,Malgorzata;Setola,Vincent;Raffay,Thomas;Roth,Bryan;Glennon,RichardA
对 4-(N,N-二甲基氨基甲基)-N9-芳基磺酰基-9H-1,2,3,4-四氢咔唑（苯磺酰色胺 5-HT6 拮抗剂 MS-245 的构象限制类似物）与人 5-HT6 受体结合的结构-亲和关系的研究表明，各种芳基磺酰基取代基是可以耐受的，并且结合不需要 4-(N,N-二甲基氨基甲基) 基团。特别是，N9-(4-氨基苯磺酰基)-9H-1,2,3,4-四氢咔唑 (20，Ki=29 nM) 被发现以高亲和力结合，代表具有 5-HT6 拮抗剂特性的新结构类别的第一个成员（pA2=7.0；cAMP 水解测定）。
An investigation of the structure–affinity relationships for the binding of 4-(N,N-dimethylaminomethyl)-N9-arylsulfonyl-9H-1,2,3,4-tetrahydrocarbazoles (conformationally-constrained analogues of the benzenesulfonyltryptamine 5-HT6antagonist MS-245) at human 5-HT6receptors revealed that various arylsulfonyl substituents are tolerated and that the 4-(N,N-dimethylaminomethyl) group is not required for binding. In particular, N9-(4-aminobenzenesulfonyl)-9H-1,2,3,4-tetrahydrocarbazole (20, Ki=29 nM) was found to bind with high affinity and represents the first member of a new structural class of agents with 5-HT6antagonist properties (pA2=7.0; cAMP hydrolysis assay).