中文名：盐酸他克林水合物

9-氨基-1,2,3,4-四氢吖啶 盐酸盐 水合物

英文名：Tacrine hydrochloride hydrate

9-Amino-1,2,3,4-tetrahydroacridine hydrochloride hydrate

CAS号：206658-92-6

MDL Number：MFCD00150067

分子式：C13H17ClN2O

分子量：252.740

描述：Tacrine是胆碱酯酶（cholinesterase）抑制剂，可对抗骨骼肌松弛药的作用，可作为呼吸兴奋剂并用于阿兹海默病和其他系统障碍。它也是组胺N-甲基转移酶（histamine N-methyltransferase）抑制剂。

溶解性：DMSO : 32 mg/mL (126.61 mM; Need ultrasonic and warming)

体外研究：

Tacirne is an active cholinesterase inhibitor that blocks the degradation of cholinergic nerves in the cerebral cortex and hippocampus to increase cholinergic transmission. Tacrine induces hepatic damages in vitro. It can also induce oxidative stress and mitochondrial dysfunction. Tacrine treatment in HepG2 cells markedly inhibits the phosphorylation of GSK3β.

体内研究：In rats, tacrine increased markers of liver damages (ALT and AST), degenerative region areas, and numbers of infiltrating inflammatory cells. Tacrine is known to induce hepatocyte necrosis and degeneration. In the past, tacrine was used for the treatment of cognitive dysfunction during vascular dementia and Alzheimer disease. It is found to abolish lipopolysaccharide induced inflammation including IL-6 secretion in the central nervous system. Tacrine can aggravate the progress of tularemia in a mouse model--the effect would be beneficial in several pathologies such as neurodegenerative disorders; e.g. the positive effect of tacrine when used in therapy for Alzheimer&＃39;s disease would be attributed to its anti-inflammatory action in addition to any improvement in cognitive functions.

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