Synthesis and biological studies of novel neurotensin(8-13) mimetics

被引：25
|
作者：
Feng, HJ
Zaidi, J
Cusack, B
Richelson, E
机构：
[1] Mayo Clin Jacksonville, Neurochem Res, Jacksonville, FL 32224 USA
[2] Mayo Clin Jacksonville, Neuropsychopharmacol Res, Jacksonville, FL 32224 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2002年 / 10卷 / 12期
关键词：
D O I：
10.1016/S0968-0896(02)00342-5
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Novel neurotensin (NT) (8-13) (Arg(8)-Arg(9)-Pro(10)-Tyr(11)-Ile(12)-Leu(13)) mimetics 3, 4 were designed by adopting all intrinsic functional groups of the native neurotensin(8-13) and using a substituted indole as a template to mimic the pharmacophore of NT(8-13). Biological studies at subtype 1 of the NT receptor showed that 3 has a 55 and 580 nM binding affinity at rat and human neurotensin receptors, respectively, As a comparison. compounds 5 and 6 were also synthesized. The binding difference between 3, 4 and 5, 6 argues the importance of the carboxylic group in achieving higher potency NT(8-13) mimetics. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：3849 / 3858
页数：10
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