N,N-二乙基-4-(5-羟基螺[2H-1-苯并吡喃-2,4'-哌啶]-4-基)苯甲酰胺盐酸盐

• 常用名: N,N-二乙基-4-(5-羟基螺[2H-1-苯并吡喃-2,4'-哌啶]-4-基)苯甲酰胺盐酸盐
• 英文名: ADL5859 HCl
• CAS号: 850173-95-4
• 分子量: 428.952
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₄H₂₉ClN₂O₃
• 熔点: N/A
• 闪点: N/A

用途

ADL5859是δ-阿片受体选择性激动剂,Ki为0.8 nM,对hERG有弱抑制性。

名称

• 中文名: N,N-二乙基-4-(5-羟基螺[2H-1-苯并吡喃-2,4'-哌啶]-4-基)苯甲酰胺盐酸盐
• 英文名: N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide,hydrochloride

生物活性

• 描述: ADL5859是δ-阿片受体选择性激动剂,Ki为0.8 nM,对hERG有弱抑制性。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 阿片受体
  信号通路 >> 神经信号通路 >> 阿片受体
  研究领域 >> 神经疾病
• 参考文献:

  [1]. Nozaki C, et al. δ-Opioid Mechanisms for ADL5747 and ADL5859 Effects in Mice: Analgesia, Locomotion, and Receptor Internalization.J Pharmacol Exp Ther. 2012 Sep;342(3):799-807.

  [2]. Le Bourdonnec B, et al. Spirocyclic delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-3-hydroxy-4-(spiro[chromene-2,4'-piperidine]-4-yl) benzamide (ADL5747).J Med Chem. 2009 Sep 24;52(18):5685-702.

  [3]. Le Bourdonnec B, Windh RT, Ajello CW, Leister LK, Gu M, Chu GH, Tuthill PA, Barker WM, Koblish M, Wiant DD, Graczyk TM, Belanger S, Cassel JA, Feschenko MS, Brogdon BL, Smith SA, Christ DD, Derelanko MJ, Kutz S, Little PJ, DeHaven RN, DeHaven-Hudkins DL,

  [4]. Le Bourdonnec B et al. Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859) J Med Chem. 2008 Oct 9;51(19):5893-6.

物理化学性质

• 分子式: C₂₄H₂₉ClN₂O₃
• 分子量: 428.952
• 精确质量: 428.186676
• PSA: 61.80000
• LogP: 4.95130
• 外观性状: 粉末
• 储存条件: -20℃

英文别名

• ADL5859 HCl
• n,n-diethyl-4-(5-hydroxyspiro(2h-1-benzopyran-2,4'-piperidin)-4-yl)benzamide hydrochloride
• Benzamide, N,N-diethyl-4-(5-hydroxyspiro[2H-1-benzopyran-2,4'-piperidin]-4-yl)-, hydrochloride (1:1)
• S1139_Selleck
• N,N-Diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidin]-4-yl)benzamide hydrochloride (1:1)
• cc-30
• N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide hydrochloride
• ADL-5859