阿莫地喹

适应症药理作用用法用量生物活性靶点体外研究体内研究阿莫地喹试剂级价格

阿莫地喹

CAS号:86-42-0
英文名:Amodiaquine
中文名:阿莫地喹
CBNumber:CB8344720
分子式:C20H22ClN3O
分子量:355.86
MOL File:86-42-0.mol

阿莫地喹化学性质

熔点 :208°C
沸点 :478.0±45.0 °C(Predicted)
密度 :1.258
储存条件 :-20°C Freezer
溶解度 :DMSO (Slightly, Sonicated), Methanol (Slightly)
形态 :Solid
酸度系数(pKa) :9.43±0.50(Predicted)
颜色 :Pale Yellow to Light Yellow
CAS 数据库 :86-42-0(CAS DataBase Reference)
NIST化学物质信息 :Amodiaquine(86-42-0)

安全信息

毒害物质数据 :86-42-0(Hazardous Substances Data)
毒性 :LD50 oral in mouse: 550mg/kg

阿莫地喹性质、用途与生产工艺

适应症阿莫地喹用于治疗各种疟疾，尤其是治疗对其他抗疟药(如氯喹)产生耐药的恶性疟原虫引起的疟疾，也用于疟疾的急性发作，具有良好的耐受性。本品还可用于治疗肝阿米巴病、华支睾吸虫病、肺吸虫病、结缔组织病等，另可用于治疗光敏性疾患，如日晒红斑症。
药理作用阿莫地喹为氨基喹啉类抗疟药，是一种有效的裂殖体杀灭剂。其抗疟作用与氯喹相似，作用于红内期疟原虫，能迅速控制临床症状。本品对于抗氯喹的疟原虫也有效。
用法用量口服卫生部推荐的治疗恶性疟方案：每日顿服青蒿琥酯片200mg和阿莫地喹片600mg，连服3日。预防用每周顿服2片。治疗用首日顿服3片，第2、3日各顿服2片。
生物活性 Amodiaquine是一种合成的氨基喹啉，通过与原生动物或寄生DNA结合、阻止DNA和RNA的生成以及后续蛋白质的合成。它被用于治疗疟疾。
靶点

EC50: ~20 μM (Nurr1-LBD (ligand binding domain))
Histamine N-methyltransferase

体外研究

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.

体内研究

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.