| 中文名称 | 阿莫地喹 |
| 英文名称 | Amodiaquine |
| CAS号 | 86-42-0 |
| 分子式 | C20H22ClN3O |
| 分子量 | 355.86 |
| EINECS号 | 201-669-3 |
| 熔点 | 208°C |
| 沸点 | 478.0±45.0 °C(Predicted) |
| 密度 | 1.258 |
| 溶解度 | DMSO(轻微,超声处理),甲醇(轻微) |
| 形态 | 固体 |
| 酸度系数(pKa) | 9.43±0.50(Predicted) |
| 颜色 | 淡黄色至浅黄色 |
| 毒害物质数据 | 86-42-0(Hazardous Substances Data) |
| 毒性 | LD50 oral in mouse: 550mg/kg |
EC50: ~20 μM (Nurr1-LBD (ligand binding domain))
Histamine N-methyltransferase
Amodiaquine (10-20 μM; 4 hours) treatment suppresses LPS-induced expression of proinflammatory cytokines (IL-1β, interleukin-6, TNF-α and iNOS) in a dose-dependent manner.
Amodiaquine (5 μM; 24 hours) significantly inhibits neurotoxin (6-OHDA-induced cell death in primary dopamine cells as examined by the number of TH
+
neurons and dopamine uptake. The neuroprotective effect of Amodiaquine is also observed in rat PC12 cells.
RT-PCR
| Cell Line: | Primary microglia |
| Concentration: | 10 µM, 15 µM, 20 µM |
| Incubation Time: | 4 hours |
| Result: | Suppressed LPS-induced expression of proinflammatory cytokines (IL-1β, interleukin-6, TNF-α and iNOS) in a dose-dependent manner. |
Amodiaquine (40 mg/kg; intraperitoneal injection; daily; for 3 days; male ICR mice) treatment diminishes perihematomal activation of microglia/macrophages and astrocytes. Amodiaquine also suppresses ICH-induced mRNA expression of IL-1β, CCL2 and CXCL2, and ameliorated motor dysfunction of mice.
| Animal Model: | Male ICR mice (8-10 weeks of age) induced ntracerebral hemorrhage (ICH) |
| Dosage: | 40 mg/kg |
| Administration: | Intraperitoneal injection; daily; for 3 days |
| Result: | Diminished perihematomal activation of microglia/macrophages and astrocytes. |