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

…, MC Wirtz, CG Bashore, KE Bianco, MG Vetelino…

Index: 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 III, F. David; Schulz, David W.; Davis, Thomas I.; Sands, Steven B.; Mansbach, Robert S.; Rollema, Hans; O'Neill, Brian T. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 22 p. 4889 - 4897

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Citation Number: 71

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 ...