3,5-bicyclic aryl piperidines:: A novel class of α4β2 neuronal nicotinic receptor partial agonists for smoking cessation

被引：57

作者：

Coe, JW ^{[1
]}

Brooks, PR ^{[1
]}

Wirtz, MC ^{[1
]}

Bashore, CG ^{[1
]}

Bianco, KE ^{[1
]}

Vetelino, MG ^{[1
]}

Arnold, EP ^{[1
]}

Lebel, LA ^{[1
]}

Fox, CB ^{[1
]}

Tingley, FD ^{[1
]}

Schulz, DW ^{[1
]}

Davis, TI ^{[1
]}

Sands, SB ^{[1
]}

Mansbach, RS ^{[1
]}

Rollema, H ^{[1
]}

O'Neill, BT ^{[1
]}

机构：

[1] Pfizer Global Res & Dev, Groton Labs, Eastern Point Rd, Groton, CT 06340 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 22期

关键词：

alpha 4 beta 2 nicotinic receptor; nAChR; partial agonist; smoking cessation; alkaloid; varenicline;

D O I：

10.1016/j.bmcl.2005.08.035

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

3,5-Bicyclic aryl piperidines are a new class of high-affinity alpha 4 beta 2 nicotinic receptor agents. We have sought nicotinic receptor partial agonists of the alpha 4 beta 2 nicotinic acetylcholine receptor for smoking cessation, and a number of compounds fulfill potency, selectivity, and efficacy requirements in vitro. In vivo, selected agents demonstrate potent partial agonist efficacy on the mesolimbic doparnine system, a key measure of therapeutic potential for smoking cessation. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：4889 / 4897

页数：9

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