3,5-Bicyclic aryl piperidines: a novel class of alpha4beta2 neuronal nicotinic receptor partial agonists for smoking cessation |
| |
| Authors: | Coe Jotham W Brooks Paige R Wirtz Michael C Bashore Crystal G Bianco Krista E Vetelino Michael G Arnold Eric P Lebel Lorraine A Fox Carol B Tingley F David Schulz David W Davis Thomas I Sands Steven B Mansbach Robert S Rollema Hans O'Neill Brian T |
| |
| Institution: | Pfizer Global Research and Development, Groton Laboratories, Eastern Point Road, Groton, CT 06340, USA. jwcoe@pfizer.com |
| |
| Abstract: | 3,5-Bicyclic aryl piperidines are a new class of high-affinity alpha4beta2 nicotinic receptor agents. We have sought nicotinic receptor partial agonists of the alpha4beta2 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 dopamine system, a key measure of therapeutic potential for smoking cessation. |
| |
| Keywords: | |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ |
|
