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

被引：26

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

页码：3849 / 3858

页数：10

共 35 条

[1]

CARRAWAY R, 1976, J BIOL CHEM, V251, P7045

[2]

CARRAWAY R, 1973, J BIOL CHEM, V248, P6854

[3]

Carraway R. L., 1975, PEPTIDES CHEM STRUCT, P679

[4] NEUROTENSIN - ANTINOCISPONSIVE ACTION IN RODENTS [J].