Varenicline: an alpha4beta2 nicotinic receptor partial agonist for smoking cessation

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 pur...

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Veröffentlicht in:	Journal of medicinal chemistry 2005-05, Vol.48 (10), p.3474-3477
Hauptverfasser:	Coe, Jotham W, Brooks, Paige R, Vetelino, Michael G, Wirtz, Michael C, Arnold, Eric P, Huang, Jianhua, Sands, Steven B, Davis, Thomas I, Lebel, Lorraine A, Fox, Carol B, Shrikhande, Alka, Heym, James H, Schaeffer, Eric, Rollema, Hans, Lu, Yi, Mansbach, Robert S, Chambers, Leslie K, Rovetti, Charles C, Schulz, David W, Tingley, 3rd, F David, O'Neill, Brian T
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Benzazepines - chemical synthesis Benzazepines - chemistry Benzazepines - pharmacology Cell Line Cerebral Cortex - drug effects Cerebral Cortex - metabolism Humans In Vitro Techniques Nicotinic Agonists - chemical synthesis Nicotinic Agonists - chemistry Nicotinic Agonists - pharmacology Oocytes - drug effects Oocytes - physiology Quinoxalines - chemical synthesis Quinoxalines - chemistry Quinoxalines - pharmacology Radioligand Assay Rats Receptors, Nicotinic - drug effects Receptors, Nicotinic - physiology Smoking Cessation - methods Varenicline Xenopus laevis
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