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Hexamethonium-type allosteric modulators of the muscarinic receptors bearing lateral dibenzazepine moieties
Li, RT; Trankle, C; Mohr, K; Holzgrabe, U
关键词Allosteric Modulators M-2 Receptors Hexamethonium Derivatives
刊名ARCHIV DER PHARMAZIE
2001-04-01
334期:4页:121-124
收录类别SCI ; IC
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Medicinal ; Chemistry, Multidisciplinary ; Pharmacology & Pharmacy
研究领域[WOS]Pharmacology & Pharmacy ; Chemistry
关键词[WOS]ACETYLCHOLINE-RECEPTORS ; M-2 RECEPTORS ; SITE ; BINDING ; LIGANDS ; SEARCH
英文摘要

Alkane-bisammonium compounds carrying lateral phthalimido substituents are known to have a high affinity for the allosteric binding site of the acetylcholine M-2 receptor. The purpose of this study was to replace the lateral phthalimido moieties with rigid tricyclic skeletons of a large volume in order to learn more about the unction of the lateral heterocycles. In addition, methyl groups were introduced into the lateral connecting chains. Allosteric inhibition of the dissociation of [H-3]N-methylscopolamine from the :M-2 receptors in porcine cardiac homogenates served to indicate binding of the test compounds to the allosteric site. The phthalimido groups could be replaced with dibenzazepine moieties without any loss in potency. Interestingly, the additional methyl group in the lateral spacer seems to have a significant influence on the allosteric behaviour.

语种英语
WOS记录号WOS:000168559500003
引用统计
被引频次:7[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/57737
专题北京大学药学院
作者单位1.Univ Wurzburg, Inst Pharm & Food Chem, D-97074 Wurzburg, Germany
2.Beijing Med Univ, Sch Pharmaceut Sci, Dept Organ Chem, Beijing 100083, Peoples R China
3.Univ Bonn, Inst Pharm, D-53121 Bonn, Germany
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GB/T 7714
Li, RT,Trankle, C,Mohr, K,et al. Hexamethonium-type allosteric modulators of the muscarinic receptors bearing lateral dibenzazepine moieties[J]. ARCHIV DER PHARMAZIE,2001,334(4):121-124.
APA Li, RT,Trankle, C,Mohr, K,&Holzgrabe, U.(2001).Hexamethonium-type allosteric modulators of the muscarinic receptors bearing lateral dibenzazepine moieties.ARCHIV DER PHARMAZIE,334(4),121-124.
MLA Li, RT,et al."Hexamethonium-type allosteric modulators of the muscarinic receptors bearing lateral dibenzazepine moieties".ARCHIV DER PHARMAZIE 334.4(2001):121-124.
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