Varenicline: An α4β2 Nicotinic Receptor Partial Agonist for Smoking Cessation
Journal of Medicinal Chemistry2005Vol. 48(10), pp. 3474–3477
Citations Over TimeTop 1% of 2005 papers
Jotham W. Coe, Paige R. Brooks, Michael G. Vetelino, Michael Wirtz, Eric P. Arnold, Jianhua Huang, Steven B. Sands, Thomas I. Davis, Lorraine A. Lebel, Carol B. Fox, Alka Shrikhande, James 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.
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