伐尼克兰：一种用于戒烟的α4β2烟碱型受体部分激动剂。
Varenicline: an alpha4beta2 nicotinic receptor partial agonist for smoking cessation.
作者信息
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 F David, O'Neill Brian T
机构信息
Pfizer Global Research and Development, Groton Laboratories, Eastern Point Road, Groton, Connecticut 06340, USA.
出版信息
J Med Chem. 2005 May 19;48(10):3474-7. doi: 10.1021/jm050069n.
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.
在此，我们描述了一系列新型化合物，从中鉴定出用于戒烟的伐尼克兰（1,6,7,8,9 - 六氢 - 6,10 - 亚甲基 - 6H - 吡嗪并[2,3 - h][3]苯并氮杂卓）。神经元烟碱型乙酰胆碱受体（nAChRs）介导尼古丁产生依赖的作用。我们一直在寻找α4β2烟碱受体部分激动剂，以抑制吸烟产生的多巴胺能激活，同时缓解戒烟尝试时伴随的渴望和戒断综合征。伐尼克兰表现出高α4β2 nAChR亲和力和理想的体内多巴胺能特征。
Zotero 插件