Synthesis and evaluation of phenylcarbamate derivatives as ligands for nicotinic acetylcholine receptors

被引：15

作者：

Gündisch, D ^{[1
]}

Andrä, M ^{[1
]}

Munoz, L ^{[1
]}

Tilotta, MC ^{[1
]}

机构：

[1] Rhein Friedr Wilhelm Univ, Dept Pharmaceut Chem, D-53115 Bonn, Germany

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2004年 / 12卷 / 18期

关键词：

phenylcarbamate; nicotinic acetylcholine receptor; epibatidine; MLA (methyllycaconitine);

D O I：

10.1016/j.bmc.2004.06.041

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：

Phenylcarbamate derivatives were synthesized and evaluated in radioligand binding assays for different nicotinic acetylcholine receptor (nAChR) subtypes. Carbamate derivatives bearing a pyrrolidine or piperidine moiety 8-20 exhibited much lower affinity for alpha7* nAChR than the analogues in the quinuclidine series 21-25, although the same structural elements are present. Furthermore, in contrast to the quinuclidine analogues 21-25, all (S)-pyrrolidine derivatives 8-12 and the piperidine analogues 15 and 16 exhibited higher affinities for alpha4beta2* nAChR. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：4953 / 4962

页数：10

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