| 中文名称 | 哈尔碱盐酸盐(水合) |
| 英文名称 | HARMINE HYDROCHLORIDE |
| CAS号 | 343-27-1 |
| 分子式 | C13H13ClN2O |
| 分子量 | 248.71 |
| EINECS号 | 206-443-8 |
| 熔点 | 265-270°C |
| LogP | 3.173 (est) |
| 溶解度 | 溶于水(高达 25 mg/ml)。 |
| 形态 | 粉末 |
| 颜色 | 灰白色至淡绿色 |
| 默克索引编号 | 14,4616 |
| 稳定性 | 可在-20°下蒸馏水溶液保存长达3个月。 |
| 危险品标志 | Xn |
| 危险类别码 | 20/21/22-40 |
| 安全说明 | 22-36 |
| 危险品运输编号 | 1544 |
| WGK Germany | 3 |
| RTECS号 | MG9450000 |
| 海关编码 | 29339900 |
| 危险等级 | 6.1(b) |
| 包装类别 | III |
| Target | Value |
|
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 |
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.
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.