bis(7)-Tacrine

bis(7)-Tacrine用途

双(7)-盐酸他克林是从他克林衍生的二聚体乙酰胆碱酯酶抑制剂。双(7)-盐酸他克林通过阻断NMDA受体防止谷氨酸诱导的神经元凋亡。双(7)-盐酸他克林是一种有效的GABA受体拮抗剂。双(7)-盐酸他克林具有研究阿尔茨海默病的潜力[1][2][3]。

bis(7)-Tacrine名称

[ CAS 号 ]:
224445-12-9

[ 中文名 ]:
bis(7)-Tacrine

[ 英文名 ]:
BIS(7)-TACRINE

[英文别名 ]:

Tacrine-Based Inhibitor 2f

bis(7)-Tacrine生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 神经信号通路 >> iGluR

信号通路 >> 跨膜转运 >> GABA受体

研究领域 >> 神经疾病

信号通路 >> 神经信号通路 >> GABA受体

信号通路 >> 跨膜转运 >> iGluR

信号通路 >> 神经信号通路 >> 疼痛

[参考文献]

[1]. Li XY, et al. Actions of bis(7)-tacrine and tacrine on transient potassium current in rat DRG neurons and potassium current mediated by K(V)4.2 expressed in Xenopus oocyte. Brain Res. 2010;1318:23-32.

[2]. Li CY, et al. Bis(7)-tacrine, a novel dimeric AChE inhibitor, is a potent GABA(A) receptor antagonist. Neuroreport. 1999;10(4):795-800.

[3]. Luo J, et al. Novel dimeric bis(7)-tacrine proton-dependently inhibits NMDA-activated currents. Biochem Biophys Res Commun. 2007;361(2):505-509.

bis(7)-Tacrine物理化学性质

[ 分子式 ]:
C₃₃H₄₂Cl₂N₄

[ 分子量 ]:
565.619

[ 精确质量 ]:
564.278625

[ PSA ]:
49.84000

[ LogP ]:
9.76510

[ 储存条件 ]:
-20°C，密闭，干燥

bis(7)-Tacrine安全信息

[ 危害码 (欧洲) ]:
T: Toxic;

[ 风险声明 (欧洲) ]:
25-36/37/38

[ 安全声明 (欧洲) ]:
26-36-45

[ 危险品运输编码 ]:
UN 2811 6.1/PG 3

bis(7)-Tacrine文献

Synthesis of alkylene linked bis-THA and linked benzyl-THA as highly potent and selective inhibitors and molecular probes of acetylcholinesterase. Pang, et al.

J. Chem. Soc. Perkin Trans. I , 171, (1997)

Highly potent, selective, and low cost bis-tetrahydroaminacrine inhibitors of acetylcholinesterase. Steps toward novel drugs for treating Alzheimer's disease.

J. Biol. Chem. 271 , 23646, (1996)

We report highly potent, selective, and low cost bifunctional acetylcholinesterase (AChE) inhibitors developed by our two-step prototype optimization strategy utilizing computer modeling of ligand doc...

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