64821-19-8
中文名稱
化合物MAO-IN-M30二鹽酸鹽
英文名稱
VAR10300 dihydrochloride
CAS
64821-19-8
分子式
C14H16Cl2N2O
分子量
299.196
MOL 文件
64821-19-8.mol
更新日期
2024/12/22 16:36:06
64821-19-8 結(jié)構(gòu)式
基本信息
中文別名
化合物MAO-IN-M30二鹽酸鹽 英文別名
M30 dihydrochlorideM-30 dihydrochloride
VAR10300 dihydrochloride
MAO-IN-M30 dihydrochloride
5-[[Methyl(2-propyn-1-yl)amino]methyl]-8-quinolinol Dihydrochloride
5-[N-methyl-N-propargylaminomethyl]-8-hydroxyquinoline dihydrochloride
N-(8-Hydroxy-5-quinolylmethyl)-N-methyl-2-propynylamine dihydrochloride
安全數(shù)據(jù)
常見問題列表
生物活性
MAO-IN-M30 dihydrochloride 是一種口服活性，可通過血腦屏障的，腦選擇性不可逆 MAO-A (IC50=37 nM) 和 MAO-B (IC50=57 nM) 抑制劑。MAO-IN-M30 dihydrochloride 是有效的鐵螯合劑、自由基清除劑。MAO-IN-M30 dihydrochloride 對(duì) Dexamethasone 誘導(dǎo)的腦細(xì)胞凋亡具有神經(jīng)保護(hù)作用。MAO-IN-M30 dihydrochloride 在 MPTP 和 lactacystin 帕金森病模型中也顯示出神經(jīng)恢復(fù)活性。靶點(diǎn)
|
MAO-A 37 nM (IC 50 ) |
MAO-B 57 nM (IC 50 ) |
體外研究
MAO-IN-M30 (0.25 nM; 72 hours) significantly increased cell viability to ~90% after exposure to Dexamethasone.
MAO-IN-M30 (0-10 μM; 24 hours) enhances PC12 cell survival.
MAO-IN-M30 treatment significantly decreases the occurrence of fragmented DNA compared to the dexamethasone-treated group in SH-SY5Y cells.
Cell Viability Assay
| Cell Line: | SH-SY5Y cells |
| Concentration: | 0.25?nM |
| Incubation Time: | 72 hours |
| Result: | Significantly increased cell viability to ～90% after exposure to Dexamethasone. |
Cell Viability Assay
| Cell Line: | PC12 cells |
| Concentration: | 0-10 μM |
| Incubation Time: | 24 hours |
| Result: | Enhanced the PC12 cell viability, the cell viability increasing to 85 ± 6 and 90 ± 7%. |
體內(nèi)研究
MAO-IN-M30 (0.5-2.5 mg/kg; p.o.; once daily for 14 consecutive days) possesses neuroprotective activities.
| Animal Model: | Male C57/BL mice (20-22 g; MPTP-induced neurotoxicity in mice) |
| Dosage: | 0.5, 2.5 mg/kg |
| Administration: | P.o.; once daily for 14 consecutive days |
| Result: | Significantly elevate striatal dopamine levels, reduce its metabolism, and elevate tyrosine-hydroxylase protein levels and activity. Elevated MPTP-reduced dopaminergic and transferrin receptor cell count in the SNpc. |