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哈尔碱盐酸盐(水合)

更新时间: 2024-09-26 20:48:21 责编:网友投稿 浏览

哈尔碱盐酸盐(水合)

哈尔碱盐酸盐(水合) 用途与合成方法
生物活性Harmine (Telepathine)是属于β-咔啉家族化合物的一种荧光harmala生物碱,是一种高细胞渗透性的 DYRK1A 的激酶口袋结合ATP的竞争性抑制剂,与DYRK2结合IC50值高约60倍。Harmine 还可以抑制 monoamine oxidases (MAOs) 和 cdc-like kinases (CLKs)。Harmine 抑制 5-HT2A serotonin receptor 的Ki值为397 nM。
靶点
TargetValue
DYRK1A
(Cell-free assay)
33 nM
MNB
(Cell-free assay)
149 nM
DYRK1B
(Cell-free assay)
166 nM
DYRK2
(Cell-free assay)
1.9 μM
体外研究

Harmine inhibits tau phosphorylation by DYRK1A by selected DANDYs, with an IC 50 of 190 nM. Harmine negatively regulates homologous recombination (HR) by interfering Rad51 recruitment, resulting in severe cytotoxicity in hepatoma cells. Furthermore, NHEJ inhibitor Nu7441 markedly sensitizes Hep3B cells to the anti-proliferative effects of Harmine.

体内研究

It is shown that brain water content is significantly increased in the TBI group. Treatment with Harmine significantly reduces the tissue water content at 1, 3 and 5 days, compared with the TBI group. Harmine treatment significantly reduces the escape latency at 3 and 5 days, compared with the TBI group. Post-TBI administration of Harmine significantly improves the motor function recovery of the rats at 1, 3 and 5 days following TBI, compared with the TBI group without Harmine treatment. The neuronal survival rate in the Harmine-treated group is significantly increased, compared with the TBI group. Administration of Harmine results in marked elevation in the expression of GLT-1, compared with the TBI group. The administration of Harmine significantly reduces the expression of caspase 3, compared with the TBI group.

化学性质 黄色结晶粉末,可溶于甲醇、乙醇、DMSO等有机溶剂,来源于骆驼蓬。
用途 盐酸去氢骆驼蓬碱具有抗肿瘤的作用。
用途 用于含量测定/鉴定/药理实验等。
药理药效:杀菌、止痒,抗银屑病作用,抗肿瘤作用。
类别有毒物质
毒性分级高毒
急性毒性静脉- 小鼠 LD50: 38 毫克/公斤
可燃性危险特性可燃, 燃烧时分解有毒氯化物, 氮氧化物气体
储运特性库房低温, 通风, 干燥; 与食品原料分开存放
灭火剂水, 二氧化碳, 泡沫, 砂土
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