1,2,3,4-tetrahydrocarbazoles as 5-HT6 serotonin receptor ligands

被引：44

作者：

Chang-Fong, J

Rangisetty, JB

Dukat, M

Setola, V

Raffay, T

Roth, B

Glennon, RA ^{[1
]}

机构：

[1] Virginia Commonwealth Univ, Sch Pharm, Dept Med Chem, Richmond, VA 23298 USA

[2] Case Western Reserve Univ, Sch Med, Dept Psychiat, Cleveland, OH 44106 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 08期

关键词：

D O I：

10.1016/j.bmcl.2004.01.071

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

An investigation of the structure-affinity relationships for the binding of 4-(N, N-dimethylaminomethyl)-N-9-arylsulfonyl-9H-1,2,3,4-tetrahydrocarbazoles (conformationally-constrained analogues of the benzenesulfonyltryptamine 5-HT6 antagonist MS245) at human 5-HT6 receptors revealed that various arylsulfonyl substituents are tolerated and that the 4- (N, N-dimethyl aminomethyl) group is not required for binding. In particular, N-9-(4-aminobenzenesulfonyl)-9H-1,2,3,4-tetrahydrocarbazole (20, K-i = 29 nM) was found to bind with high affinity and represents the first member of a new structural class of agents with 5-HT6 antagonist properties (pA(2) = 7.0; cAMP hydrolysis assay). (C) 2004 Elsevier Ltd. All rights reserved.

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页码：1961 / 1964

页数：4

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