634616-95-8

• 常用中文名：TBPB
• 常用英文名：TBPB
• CAS号：634616-95-8
• 分子式：C₂₅H₃₂N₄O
• 分子量：404.548
• 相关类别： 信号通路 G 蛋白偶联受体/G 蛋白 由mAChR
• 发布时间：2017-10-12 15:43:39
• 更新时间：2024-01-02 09:27:01
• TBPB是M1 mAChR变构激动剂,EC50值为289nM,调节amyloid的加工和小鼠体内具有抗精神病药物等活性。

名称

• 中文名: TBPB
• 英文名: 1-[1'-(2-Methylbenzyl)-1,4'-bipiperidin-4-yl]-1,3-dihydro-2H-benz imidazol-2-one
• 英文别名: 2H-Benzimidazol-2-one, 1,3-dihydro-1-[1'-[(2-methylphenyl)methyl][1,4'-bipiperidin]-4-yl]-; 2-Pyrrolo-1,3,2-dioxa-phospholan; 1-[1'-(2-Methylbenzyl)-1,4'-bipiperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one; 2-pyrrol-1-yl-1,3,2-dioxaphospholan; TBPB

物化性质

• 密度: 1.2±0.1 g/cm3
• 分子式: C₂₅H₃₂N₄O
• 分子量: 404.548
• 精确质量: 404.257599
• PSA: 44.53000
• LogP: 4.96
• 折射率: 1.623
• 储存条件: 2-8℃

生物活性

• 描述: TBPB是M1 mAChR变构激动剂,EC50值为289nM,调节amyloid的加工和小鼠体内具有抗精神病药物等活性。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 由mAChR
  信号通路 >> 神经信号通路 >> mAChR
  研究领域 >> 神经疾病
• 参考文献:

  [1]. Jones CK, et al. Novel selective allosteric activator of the M1 muscarinic acetylcholine receptor regulates amyloid processing and produces antipsychotic-like activity in rats. J Neurosci. 2008 Oct 8;28(41):10422-33.

  [2]. Miller NR, et al. Synthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas--the effect of capping the distal basic piperidine nitrogen. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5443-7.

安全

• 危险品运输编码: NONH for all modes of transport

合成路线

20662-53-7 76167-41-4 ~75% 634616-95-8

文献：Rasheed, Mohammed Abdul; Shaik, Nagul Meera; Nirogi, Ramakrishna Synthetic Communications, 2013 , vol. 43, # 13 p. 1796 - 1801

1074762-36-9 20662-53-7 ~82% 634616-95-8

文献：Bridges, Thomas M.; Brady, Ashley E.; Phillip Kennedy; Nathan Daniels; Miller, Nicole R.; Kim, Kwango; Breininger, Micah L.; Gentry, Patrick R.; Brogan, John T.; Jones, Carrie K.; Jeffrey Conn; Lindsley, Craig W. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 20 p. 5439 - 5442

79099-07-3 ~% 634616-95-8

文献：Rasheed, Mohammed Abdul; Shaik, Nagul Meera; Nirogi, Ramakrishna Synthetic Communications, 2013 , vol. 43, # 13 p. 1796 - 1801

95-54-5 ~% 634616-95-8

文献：Rasheed, Mohammed Abdul; Shaik, Nagul Meera; Nirogi, Ramakrishna Synthetic Communications, 2013 , vol. 43, # 13 p. 1796 - 1801

79099-00-6 ~% 634616-95-8

文献：Rasheed, Mohammed Abdul; Shaik, Nagul Meera; Nirogi, Ramakrishna Synthetic Communications, 2013 , vol. 43, # 13 p. 1796 - 1801

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