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.
引用
收藏
页码：1987 / 1991
页数：5
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