中文名：鹽酸他克林水合物

      9-氨基-1,2,3,4-四氫吖啶 鹽酸鹽 水合物

英文名：Tacrine hydrochloride hydrate

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

CAS號(hào)：206658-92-6

MDL Number：MFCD00150067

分子式：C13H17ClN2O

分子量：252.740

結(jié)構(gòu)式：

描述：Tacrine是cholinesterase抑制劑，可對(duì)抗骨骼肌松弛藥的作用，可作為呼吸劑并用于阿茲海默病和其他系統(tǒng)障礙。它也是組胺N-甲基轉(zhuǎn)移酶（histamine N-methyltransferase）抑制劑。

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

體外研究：

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.

體內(nèi)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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