盐酸阿莫地喹

中文名称:

盐酸阿莫地喹

中文同义词:

阿莫地喹碱;盐酸阿莫他喹;阿莫地喹盐酸盐;盐酸阿莫地喹;7-氯-4-(3-二乙基氨基甲基-4-羟基苯胺基)喹啉二盐酸盐;阿莫他喹二盐酸盐;阿莫地喹二盐酸盐;4-((7-氯喹啉-4-基)氨基)-2-((二乙胺基)甲基)苯酚二盐酸盐

英文名称:

Acrichin dihydrochloride

英文同义词:

4-[(7-CHLORO-4-QUINOLINYL)AMINO]-2-[(DIETHYLAMINO)METHYL]PHENOL DIHYDROCHLORIDE;AMODIAQUIN DIHYDROCHLORIDE;AMODIAQUIN HYDROCHLORIDE;AMODIAQUINE HYDROCHLORIDE;AMODIAQUINE HCL;AMODIAQUINE DIHYDROCHLORIDE;4-((7-chloro-4-quinolyl)amino)-alpha-(diethylamino)-o-cresodihydrochloride;4-((7-chloro-4-quinolyl)amino)-alpha-(diethylamino)-o-cresoldihydrochloride

CAS号:

69-44-3

分子式:

C20H23Cl2N3O

分子量:

392.32

EINECS号:

200-706-0

相关类别:

化工原料;植提;医药原料;添加剂;原料;API

Mol文件:

69-44-3.mol

储存条件 

Sealed in dry,Room Temperature

药物相互作用

1. 与其它抗疟药同时使用粒性细胞缺乏症发生率较高。 2. 与三硅酸镁和白陶土同时服用，氯喹胃肠吸收下降，阿莫地喹可能同氯喹相同。 3. 皮下注射狂犬病疫苗的同时服用氯喹预防疟疾时，可能会干扰抗体的产生。在使用阿莫地喹时应考虑。

注意事项

阿莫地喹的临床前研究就估计到了它的诱变和遗传毒性效应。细菌诱变的实验报告显示，对沙门菌属的诱变作用很弱，但对妊娠期服用阿莫地喹的剂量还没有研究，也就没有引起器官和结构畸形的数据资料。有资料显示，在妊娠期服用氯喹后出现了几例先天畸形（法洛四联症、先天性甲状腺功能减退、脉络膜视网膜炎耳聋），氯喹能通过胎盘屏障，阿莫地喹可能也可以通过，但在妊娠期使用阿莫地喹药物没有发现先天畸形。尽管这样，有研究者认为妊娠期应禁用阿莫地喹。而其他的研究者认为即使没有足够的资料显示阿莫地喹的安全 性，但是在没有找到可替代的药物之前不应该限制它的使用。WHO 也认识到了阿莫地喹的毒性，但没有在妊娠期禁用阿莫地喹的数据，因此需要进一步的研究。

生物活性

Amodiaquine dihydrochloride (Amodiaquin dihydrochloride) 是一种4-氨基喹啉类抗疟剂，是一种有效的具有口服活性的组胺 N-甲基转移酶 (histamine N-methyltransferase) 抑制剂，Ki 值为 18.6 nM。Amodiaquine dihydrochloride 也是一种 Nurr1 激动剂，可特异性结合 Nurr1 的配体结合域，EC50 为 ~20 μM。抗炎作用。

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.

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.

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.

WGK Germany 

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