Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1378188 | Bioorganic & Medicinal Chemistry Letters | 2005 | 9 Pages |
Abstract
3,5-Bicyclic aryl piperidines are a new class of high-affinity α4β2 nicotinic receptor agents. We have sought nicotinic receptor partial agonists of the α4β2 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.
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Related Topics
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Chemistry
Organic Chemistry
Authors
Jotham W. Coe, Paige R. Brooks, Michael C. Wirtz, Crystal G. Bashore, Krista E. Bianco, Michael G. Vetelino, Eric P. Arnold, Lorraine A. Lebel, Carol B. Fox, F. David Tingley III, David W. Schulz, Thomas I. Davis, Steven B. Sands, Robert S. Mansbach,