249296-44-4

• 常用中文名：伐尼克兰
• 常用英文名：Varenicline
• CAS号：249296-44-4
• 分子式：C₁₃H₁₃N₃
• 分子量：211.26
• 相关类别： 信号通路 跨膜转运 胆碱受体
• 发布时间：2018-08-07 11:17:07
• 更新时间：2026-07-04 22:22:22

名称

• 中文名: 伐伦克林
• 英文名: varenicline
• 中文别名: 伐伦克林/伐尼克兰; 伐伦克林酒石酸; 瓦伦尼克林; 伐尼克兰杂质(全套); 7,8,9,10-四氢-6,10-亚甲基-6H-吡嗪并[2,3-h]苯并氮杂卓; 伐仑克林(戒烟); 伐尼克林; 伐尼克兰杂质; 7,8,9,10-四氢-6H-6,10-甲桥氮杂卓并[4,5-g]喹喔啉; 酒石酸伐仑克林(戒烟); Venicline (伐尼克兰); 7,8,9,10-四氢-6,10-亚甲基-6H-吡嗪并[2,3-h][3]苯并氮杂卓; 伐伦克林游离碱; 伐尼游离碱
• 英文别名: Vareniclene; 7,8,9,10-tetrahydro-6H-6,10-methanoazino[4,5-g]quinoxaline; 3-h]benzazine; Hsdb; 7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino[2,3-h]benzazine (Veniclene); 5,8,14-triazatetracycIo[10.3.1.0(2,11).0(4,9)]hexadeca-2(11),3,5,7,9-pentaene; 7,8,9,10-tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine; Venicline Impurity; (1R,12S)-5,8,14-triazatetracyclo[10.3.1.0^{2,11}.0^{4,9}]hexadeca-2,4,5,7,10-pentaene; Venicline; 5,8,14-triazatetracyclo[10.3.1.0(2,11).0(4,9)]hexadeca-2(11),3,5,7,9-pentaene; Veniclene; 3-h][3]benzazepine; Venicline free base; (6R,10S)-7,8,9,10-tetrahydro-6H-6,10-methanoazino[4,5-g]quinoxaline; Vanni free base; Venicline 13C15N; (1R,12S)-5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca-2,4,6,8,10-pentaene; Unii-W6hs99o8zo; 7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino[2,3-h]benzazine; 10-tetrahydro; Venicline base; Vancomycin Impurity 20; 5,8,14-triazatetracyclo[10.3.1.0(2,11),0(4,9)]hexadeca-2(l11),3,5,7,9-pentaene; Venciline; 6,10-Methano-6H-pyrazino[2,3-h]benzazine, 7,8,9,10-tetrahydro; Chantix; 10-Methano-6H-pyrazino[2; 526555;CHAMPIX;CHANTIX;526555;-526555; VERENICLINE

物化性质

• 密度: 1.247g/cm3
• 沸点: 400.6ºC at 760mmHg
• 分子式: C₁₃H₁₃N₃
• 分子量: 211.26
• 闪点: 196.1ºC
• PSA: 152.87000
• LogP: 0.01010
• 蒸汽压: 1.25E-06mmHg at 25°C
• 折射率: 1.667
• 储存条件: 2-8℃

生物活性

• 相关类别:
  信号通路 >> 跨膜转运 >> 胆碱受体
  信号通路 >> 神经信号通路 >> 胆碱受体
  研究领域 >> 神经疾病
• 参考文献:

  [1]. Kikkawa, H.; Maruyama, N.; Fujimoto, Y.; Hasunuma, T. Single- and multiple-dose pharmacokinetics of the selective nicotinic receptor partial agonist, varenicline, in healthy Japanese adult smokers. Journal of Clinical Pharmacology (2011), 51(4), 527-537.

  [2]. Bordia T, Hrachova M, Chin M et al. Varenicline Is a Potent Partial Agonist at α6β2* Nicotinic Acetylcholine Receptors in Rat and Monkey Striatum. J Pharmacol Exp Ther. 2012 Aug;342(2):327-34.

  [3]. Pachas GN, Cather C, Pratt SA et al. Varenicline for Smoking Cessation in Schizophrenia: Safety and Effectiveness in a 12-Week, Open-Label Trial. J Dual Diagn. 2012;8(2):117-125.

  [4]. Krebs P, Sherman SE. Review: Varenicline for tobacco cessation does not increase CV serious adverse events. Ann Intern Med. 2012 Aug 21;157(4):JC2-2.

合成路线

1333145-92-8 ~83% 249296-44-4

文献：Teva Pharmaceutical Industries Ltd. Patent: US2010/324055 A1, 2010 ; Location in patent: Page/Page column 4-5 ;

1333146-06-7 ~68% 249296-44-4

文献：Teva Pharmaceutical Industries Ltd. Patent: US2010/324055 A1, 2010 ; Location in patent: Page/Page column 5 ;

1186072-37-6 ~61% 249296-44-4

文献：Teva Pharmaceutical Industries Ltd. Patent: US2010/324055 A1, 2010 ; Location in patent: Page/Page column 5 ;

1197286-22-8 ~96% 249296-44-4

文献：TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC. Patent: WO2009/143347 A2, 2009 ; Location in patent: Page/Page column 25 ;

1206484-38-9 ~65% 249296-44-4

文献：Pasikanti, Srinivas; Srinivasa Reddy; Venkatesham; Dubey; Iqbal, Javed; Das, Parthasarathi Tetrahedron Letters, 2010 , vol. 51, # 1 p. 151 - 152

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