| Literature DB >> 15887955 |
Jotham W Coe1, Paige R Brooks, Michael G Vetelino, Michael C Wirtz, Eric P Arnold, Jianhua Huang, Steven B Sands, Thomas I Davis, Lorraine A Lebel, Carol B Fox, Alka Shrikhande, James H Heym, Eric Schaeffer, Hans Rollema, Yi Lu, Robert S Mansbach, Leslie K Chambers, Charles C Rovetti, David W Schulz, F David Tingley, Brian T O'Neill.
Abstract
Herein we describe a novel series of compounds from which varenicline (1, 6,7,8,9-tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine) has been identified for smoking cessation. Neuronal nicotinic acetylcholine receptors (nAChRs) mediate the dependence-producing effects of nicotine. We have pursued alpha4beta2 nicotinic receptor partial agonists to inhibit dopaminergic activation produced by smoking while simultaneously providing relief from the craving and withdrawal syndrome that accompanies cessation attempts. Varenicline displays high alpha4beta2 nAChR affinity and the desired in vivo dopaminergic profile.Entities:
Mesh：
Substances：
Year: 2005 PMID： 15887955 DOI： 10.1021/jm050069n
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446