生物活性 | |||
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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 | |||||
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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NCT01406522 | Cocaine Dependence | Phase 2 | Withdrawn(One of the study med...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 | |||
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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 |
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[2]Freeman SE, Dawson RM. Tacrine: a pharmacological review. Prog Neurobiol. 1991;36(4):257-77. |