| CAS |
442-51-3 |
| Chinese Name |
去氢骆驼蓬碱 |
| English Name |
Harmine |
| Synonyms |
Telepathine |
| Molecular Formula |
C13H12N2O |
| Molecular Weight |
212.25 |
| Solubility |
Soluble in DMSO |
| Purity |
HPLC≥98% |
| Appearance |
Off-white to brown Solid |
| Storage |
Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC |
EINECS 207-131-4 |
| MDL |
MFCD00004958 |
| SMILES |
CC1=NC=CC2=C1NC3=C2C=CC(OC)=C3 |
| InChIKey |
BXNJHAXVSOCGBA-UHFFFAOYSA-N |
| InChI |
InChI=1S/C13H12N2O/c1-8-13-11(5-6-14-8)10-4-3-9(16-2)7-12(10)15-13/h3-7,15H,1-2H3 |
| PubChem CID |
5280953 |
| Target Point |
DYRK;PPARγ;5-HT Receptor;MAO-A |
| Passage |
Cell Cycle;DNA Damage/DNA Repair;Metabolic Enzyme&Protease;Neuronal Signaling;GPCR & G Protein;Protein Tyrosine Kinase/RTK |
| Background |
It is a bi-specific tyrosine phosphorylated regulated kinase (DYRK) inhibitor with anti-cancer and anti-inflammatory activities. It has a high affinity for 5-HT2A serotonin receptor. PPARγ expression is regulated by inhibition of Wnt signaling pathway. It also selectively binds MAO-A and reversibly inhibits it. |
| Biological Activity |
Harmine是5-HT2A的抑制剂，Ki为397 nM [1]。 |
| In Vitro |
Harmine通过选择的DANDY抑制DYRK1A的tau磷酸化，IC50为190 nM [2] .Harmine通过干扰Rad51募集负调节HR，导致肝癌细胞的严重细胞毒性。此外，NHEJ抑制剂Nu7441显著增强Hep3B细胞对Harmine的抗增殖作用[3]。 |
| In Vivo |
结果表明，TBI组脑水含量显著增加。与TBI组相比，Harmine治疗在第1，3和5天显著降低组织水含量。与TBI组相比，Harmine治疗显著降低了3天和5天的逃避潜伏期。与没有Harmine治疗的TBI组相比，TBI后TBI给予显著改善TBI后1，3和5天大鼠的运动功能恢复。与TBI组相比，Harmine治疗组的神经元存活率显著增加。与TBI组相比，给予Harmine导致GLT-1表达显著升高。与TBI组相比，Harmine的给药显著降低了caspase 3的表达[4]。 |
| Animal Experiment |
大鼠[4]共150只雄性Sprague-Dawley大鼠(年龄10-12周;体重280-320g;用于本研究。大鼠随机分为三组：假手术组(假手术组); n = 15); TBI组(TBI; n = 35)和TBI + Harmine治疗组(Harmine; n = 35)。在TBI(ip，30 mg/kg/d)后立即给予Harmine用于向上假性和TBI组接受等体积的0.9％生理盐水(ip)。大鼠按如下分组进行行为恢复检查：Sham，n = 3; TBI，n = 7;和Harmine，n = 7.在TBI后，在第1，3和5天评估NSS。每只大鼠由对动物治疗不知情的观察者进行评估[4]。 |
| Data Literature Source |
[1]. Glennon RA，et al. Binding of beta-carbolines and related agents at serotonin (5-HT(2) and 5-HT(1A))，dopamine (D(2)) and benzodiazepine receptors. Drug Alcohol Depend. 2000 Aug 1;60(2):121-32.
[2]. Neumann F，et al. DYRK1A inhibition and cognitive rescue in a Down syndrome mouse model are induced by new fluoro-DANDY derivatives. Sci Rep. 2018 Feb 12;8(1):2859.
[3]. Zhang L，et al. Harmine suppresses homologous recombination repair and inhibits proliferation of hepatoma cells. Cancer Biol Ther. 2015;16(11):1585-92.
[4]. Zhong Z，et al. Treatment with harmine ameliorates functional impairment and neuronal death following traumatic brain injury. Mol Med Rep. 2015 Dec;12(6):7985-91. |
| Unit |
Bottle |
| Specification |
20mg 10mM*1mL in DMSO 100mg |
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