123464-89-1

• 常用中文名：PNU-282987
• 常用英文名：PNU 282987
• CAS号：123464-89-1
• 分子式：C₁₄H₁₈Cl₂N₂O
• 分子量：301.21
• 相关类别： 信号通路 跨膜转运 胆碱受体
• 发布时间：2018-10-15 14:13:22
• 更新时间：2024-01-02 16:14:00
• PNU-282987是_alpha_7 nAChR受体选择性激动剂,Ki值为26nM,对_alpha_1_beta_1_gamma__delta_和_alpha_3_beta_4nAChRs亲和力弱。

名称

• 中文名: N-(3R)-1-氮杂双环[2,2,2]辛-3-基-4-氯苯甲酰胺盐酸盐
• 英文名: N-(3R)-1-Azabicyclo[2.2.2]oct-3-yl-4-chlorobenzamide
• 英文别名: PNU-282987; N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-4-chlorobenzamide; Kisspeptin 234; Benzamide, N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]-4-chloro-

物化性质

• 密度: 1.3±0.1 g/cm3
• 沸点: 431.5±30.0 °C at 760 mmHg
• 分子式: C₁₄H₁₈Cl₂N₂O
• 分子量: 301.21
• 闪点: 214.8±24.6 °C
• PSA: 32.34000
• LogP: 2.49
• 蒸汽压: 0.0±1.0 mmHg at 25°C
• 折射率: 1.612
• 储存条件: 2-8℃

生物活性

• 描述: PNU-282987是_alpha_7 nAChR受体选择性激动剂,Ki值为26nM,对_alpha_1_beta_1_gamma__delta_和_alpha_3_beta_4nAChRs亲和力弱。
• 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]. Bodnar AL, et al. Discovery and structure-activity relationship of quinuclidine benzamides as agonists of alpha7 nicotinic acetylcholine receptors. J Med Chem. 2005 Feb 24;48(4):905-8.

  [2]. Li F, et al. The protective effect of PNU-282987, a selective α7 nicotinic acetylcholine receptor agonist, on the hepatic ischemia-reperfusion injury is associated with the inhibition of high-mobility group box 1 protein expression and nuclear factor κB activation in mice. Shock. 2013 Feb;39(2):197-203.

  [3]. Stuckenholz V, et al. The α7 nAChR agonist PNU-282987 reduces inflammation and MPTP-induced nigral dopaminergic cell loss in mice. J Parkinsons Dis. 2013;3(2):161-72.

  [4]. Mesa-Gresa P, et al. Behavioral effects of different enriched environments in mice treated with the cholinergic agonist PNU-282987. Behav Processes. 2014 Mar;103:117-24.

  [5]. Dong Jun Yu, et al. Effect of ischemic preconditioning combined with α7 nAchR agonists on limb ischemia-reperfusion lung injury in rat. Biomed Res. 2017; Special Issue: ISSN 0970.