A novel class of allosteric modulators of the muscarinic M2 acetylcholine receptor:: terphenyl derivatives

被引：3

作者：

Teichgräber, J ^{[1
]}

Holzgrabe, U ^{[1
]}

机构：

[1] Univ Wurzburg, Inst Pharm & Food Chem, D-97074 Wurzburg, Germany

来源：

TETRAHEDRON | 2003年 / 59卷 / 44期

关键词：

allosteric modulation; muscarinic receptors; terphenyl derivatives;

D O I：

10.1016/j.tet.2003.09.052

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The allosteric modulation of receptors has become a widely accepted concept in order to enhance the agonist or antagonist binding to a receptor. Alcuronium, characterized by a high allosteric potency and a positive cooperativity at the muscarinic M-2 receptor, was chosen as a template to design a structural novel terphenyl-type of allosteric modulator. The skeleton was build up from 1-bromo-2-methylnaphthalene and 1,4-dibromo-2,5-dimethylbenzene using bis(triphenylphosphine)nickel(II) dichloride as a catalyst. Several amino substituted terphenyls were synthesised and preliminary pharmacological tests were performed. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：8697 / 8703

页数：7

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