Varenicline: An alpha 4 beta 2 nicotinic receptor partial agonist for smoking cessation

Coe JW; Brooks PR; Vetelino MG; Wirtz MC; Arnold EP; Huang JH; Sands SB; Davis TI; Lebel LA; Fox CB

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Varenicline: An alpha 4 beta 2 nicotinic receptor partial agonist for smoking cessation

机译：瓦伦尼克碱：用于戒烟的α4β2烟碱样受体部分激动剂

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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 α 4β 2 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 α 4β 2 nAChR affinity and the desired in vivo dopaminergic profile.

机译：在本文中，我们描述了一系列新的化合物，从中确定了瓦伦尼克林（1，6,7,8,9-四氢-6,10-甲醇-6H-吡嗪并[2,3-h] [3]苯并ze庚因）已被识别出可吸烟戒烟。神经元烟碱乙酰胆碱受体（nAChRs）介导尼古丁的依赖性产生作用。我们一直在追求α4β2烟碱样受体部分激动剂，以抑制吸烟产生的多巴胺能激活，同时缓解戒烟尝试带来的渴望和戒断综合症。瓦伦尼克碱显示出高的α4β2 nAChR亲和力和所需的体内多巴胺能谱。

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来源
《Journal of Medicinal Chemistry》 |2005年第10期|共4页
作者
Coe JW; Brooks PR; Vetelino MG; Wirtz MC; Arnold EP; Huang JH; Sands SB; Davis TI; Lebel LA; Fox CB;
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正文语种 eng
中图分类药学;
关键词
ACETYLCHOLINE-RECEPTORS; BETA-2 SUBUNIT; RAT-BRAIN; CYTISINE; MECAMYLAMINE; DERIVATIVES; MECHANISMS; ADDICTION; MORTALITY; LIGANDS;

机译：乙酰胆碱受体;BETA-2亚基;大鼠脑;胱氨酸;美甲胺;衍生物;机制;成瘾;死亡率;配体;

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1. The Efficacy and Safety of Varenicline, a Selective Alpha4beta2 Nicotinic Receptor Partial Agonist, for Smoking Cessation in Patients Hospitalized With Acute Coronary Syndrome: A Randomized Controlled Trial [J] . Eisenberg Mark J., Windle Sarah B., Roy Nathalie, Circulation: An Official Journal of the American Heart Association . 2015,第23期

机译：Varenicline，选择性Alpha4beta2烟碱受体部分激动剂，对于急性冠脉综合征住院患者戒烟的疗效和安全性：一项随机对照试验。
2. Varenicline: a selective alpha4beta2 nicotinic acetylcholine receptor partial agonist approved for smoking cessation. [J] . Lam S, Patel PN Cardiology in review . 2007,第3期

机译：瓦伦尼克碱：一种批准用于戒烟的选择性α4β2烟碱型乙酰胆碱受体局部激动剂。
3. Efficacy and tolerability of varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, in a 12-week, randomized, placebo-controlled, dose-response study with 40-week follow-up for smoking cessation in Japanese smokers. [J] . Nakamura M, Oshima A, Fujimoto Y, Clinical therapeutics . 2007,第6期

机译：在一项为期12周，随机，安慰剂对照，剂量反应的研究中，对日本吸烟者进行了为期40周的随访，研究了伐尼克兰（一种α4β2烟碱乙酰胆碱受体部分激动剂）的疗效和耐受性。
4. The Alpha7-Beta2 Nicotinic Receptor and Its Roles in Amyloid Beta Pathology in Alzheimer's Disease [C] . Philip Timothy Doughty, Peace Ibole, Himgauri Vilas Naik, Southern Biomedical Engineering Conference . 2016

机译：Alpha7-Beta2烟碱受体及其在阿尔茨海默氏病的淀粉样β病理学中的作用
5. Examining the Contribution of Alpha-4 Beta-2 and Non-Alpha-4 Beta-2 Nicotinic Receptors to the in Vivo Effects of Nicotine and Varenicline. [D] . de Moura, Fernando Barreto. 2017

机译：检查Alpha-4 Beta-2和非Alpha-4 Beta-2烟碱受体对尼古丁和瓦伦尼克碱的体内作用的贡献。
6. Diverse strategies targeting alpha7 homomeric and alpha6beta2* heteromeric nicotinic acetylcholine receptors for smoking cessation [O] . Darlene H. Brunzell, J. Michael McIntosh, Roger L. Papke -1

机译：针对戒烟的α7同源和α6beta2*异聚烟碱型乙酰胆碱受体的不同策略
7. Pre-clinical properties of the alpha 4 beta 2 nicotinic acetylcholine receptor partial agonists varenicline, cytisine and dianicline translate to clinical efficacy for nicotine dependence [O] . Rollema, H., Shrikhande, A., Ward, K. M., 2010

机译：α4β2烟碱乙酰胆碱受体局部激动剂的临床前特性瓦伦尼克林，胱氨酸和二苯胺碱转化为尼古丁依赖性的临床疗效
8. Partial Primary Structure of the Alpha and Beta Chains of Human Tumor T-Cell Receptors [R] . Jones, N., Leiden, J., Dialynas, D., 1985

机译：人肿瘤T细胞受体α和β链的部分一级结构

Varenicline: An alpha 4 beta 2 nicotinic receptor partial agonist for smoking cessation

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