Tacrine HCl

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Chemical Structure| 1684-40-8 同义名 : 四氢氨基吖啶 ;Tacrine (hydrochloride); Tacrine HCl; Hydroaminacrine; C.I. 970
CAS号 : 1684-40-8
货号 : A205226
分子式 : C13H15ClN2
纯度 : 99%+
分子量 : 234.72
MDL号 : MFCD00012657
存储条件:

Pure form Inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Tacrine (Hydrochloride) is a potent inhibitor of cholinesterases and has ChE inhibitory activity and additional biological activity such as monoamine oxidase (MAO) inhibition and ion channel modulating ability. The hybrid compound containing the tryptoline moiety linked with a 7 carbon spacer to tacrine displayed the best AChE and BuChE inhibitory activity (IC50 = 17.37 and 3.16 nM)[3]. Pretreatment with tacrine can decrease cocaine-motivated behavior measured by self-administration or reinstatement, but not conditioned-place preference[4].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02292238 Alzheimer's Disease Phase 2 Recruiting November 2019 United States, New York ... 展开 >> Burke Recruiting White Plains, New York, United States, 10605 Contact: Liz Magier, MPA    914-368-3159    burkegrants@med.cornell.edu 收起 <<
NCT02821975 Depression in Remission ... 展开 >> Cognitive Computer Training Returning to Work 收起 << Not Applicable Unknown October 2017 Denmark ... 展开 >> Research Unit of Psychiatry, Psychiatric Unit Odense - University function Recruiting Odense C, Region of southern Denmark, Denmark, 5000 Contact: Anja F Elliott, BACH.MED.    +4560795724    anjaelliott@hotmail.com 收起 <<
NCT01406522 Cocaine Dependence Phase 2 Withdrawn(One of the study med... 展开 >>ications, tacrine, is no longer clinically available) 收起 << November 2013 United States, Missouri ... 展开 >> Kansas City VA Medical Center Kansas City, Missouri, United States, 64128 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.26mL

0.85mL

0.43mL

21.30mL

4.26mL

2.13mL

42.60mL

8.52mL

4.26mL

参考文献

[1]Snape MF, Misra A, et al. A comparative study in rats of the in vitro and in vivo pharmacology of the acetylcholinesterase inhibitors tacrine, donepezil and NXX-066. Neuropharmacology. 1999 Jan;38(1):181-93.

[2]Freeman SE, Dawson RM. Tacrine: a pharmacological review. Prog Neurobiol. 1991;36(4):257-77.

[3]Teponnou GAK, Joubert J, Malan SF. Tacrine, Trolox and Tryptoline as Lead Compounds for the Design and Synthesis of Multi-target Agents for Alzheimer's Disease Therapy. Open Med Chem J. 2017 Jan 31;11:24-37. doi: 10.2174/1874104501711010024. PMID: 28567126; PMCID: PMC5418947.

[4]Grasing K, Yang Y, He S. Enduring effects of tacrine on cocaine-reinforced behavior: Analysis by conditioned-place preference, temporal separation from drug reward, and reinstatement. Pharmacol Res. 2015 Jul;97:40-7. doi: 10.1016/j.phrs.2015.04.003. Epub 2015 Apr 16. PMID: 25890194; PMCID: PMC4465028.