Binding of isotryptamines and indenes at h5-HT6 serotonin receptors

被引：45

作者：

Kolanos, R

Siripurapu, U

Pullagurla, M

Riaz, M

Setola, V

Roth, BL

Dukat, M

Glennon, RA

机构：

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

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

[3] Case Western Reserve Univ, Sch Med, Dept Psychiat & Neurosci, Cleveland, OH 44106 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 08期

关键词：

serotonergic ligands; 5-HT6; binding requirements;

D O I：

10.1016/j.bmcl.2005.02.070

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

To deter-mine if the indolic nitrogen atom is required for the binding of N-1-benzyltryptamines at h5-HT6 serotonin receptors, several isotryptamines and indene analogs were examined. The affinity of 3-benzyl-N-1-(N,N-dimethylaminoethyl)indole (5, K-i = 32 nM) and 1-benzyl-3-(N,N-dimethylaminoethyl)indene (11, K-i = 3 nM) indicates that the indolic nitrogen atom is not essential for binding. (c) 2005 Elsevier Ltd. All rights reserved.

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页码：1987 / 1991

页数：5

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