盐酸阿莫地喹

盐酸阿莫地喹用途

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。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。

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盐酸阿莫地喹名称

[ CAS 号 ]:
69-44-3

[ 中文名 ]:
盐酸阿莫地喹

[ 英文名 ]:
Amodiaquine dihydrochloride

[中文别名 ]:

阿莫地喹碱

[英文别名 ]:

TCMDC-123932
camoquinhydrochloride
EINECS 200-706-0
Camoquin Hcl
AMODIAQUIN DIHYDROCHLORIDE
AMODIAQUINE HCL
AMODIAQUIN HYDROCHLORIDE
AMODIAQUINE DIHYDROCHLORIDE
AMODIAQUINE HYDROCHLORIDE

盐酸阿莫地喹生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 感染

信号通路 >> 表观遗传学 >> 组蛋白甲基转移酶

研究领域 >> 炎症/免疫

研究领域 >> 神经疾病

[ 靶点 ]

EC50: ~20 μM (Nurr1-LBD (ligand binding domain))[1] Histamine N-methyltransferase[3]

[体外研究]

阿莫地喹(10-20μM；4小时)治疗以剂量依赖性方式抑制LPS诱导的促炎性细胞因子(IL-1β、IL-6、TNF-α和iNOS)的表达[1]。阿莫地喹(5μM；24小时)显著抑制神经毒素(6-OHDA诱导的原代多巴胺细胞死亡,通过TH+神经元数量和多巴胺摄取量检测。阿莫地喹对大鼠PC12细胞也有神经保护作用[1]。RT-PCR[1]细胞系：原代小胶质细胞浓度：10µM,15µM,20µM孵育时间：4h。结果：LPS诱导的促炎性细胞因子(IL-1β、IL-6、TNF-α和iNOS)的表达呈剂量依赖性。

[体内研究]

阿莫地喹(40 mg/kg；腹腔注射；每日；连续3天；雄性ICR小鼠)治疗可减少血周小胶质细胞/巨噬细胞和星形胶质细胞的活化。阿莫地喹还可抑制脑出血诱导的IL-1β、CCL2和CXCL2的mRNA表达,改善小鼠运动功能障碍[2]。动物模型：雄性ICR小鼠(8-10周龄)诱发脊髓内出血[2]剂量：40mg/kg腹腔注射；每日；连续3天结果：血周小胶质细胞/巨噬细胞和星形胶质细胞的活化减少。

[参考文献]

[1]. Chun-Hyung Kim, et al. Nuclear receptor Nurr1 agonists enhance its dual functions and improve behavioral deficits in an animal model of Parkinson's disease. Proc Natl Acad Sci U S A. 2015 Jul 14;112(28):8756-61.

[2]. Keita Kinoshita, et al. A Nurr1 agonist amodiaquine attenuates inflammatory events and neurological deficits in a mouse model of intracerebral hemorrhage. J Neuroimmunol. 2019 May 15;330:48-54.

[3]. Akira Yokoyama, et al. Effect of amodiaquine, a histamine N-methyltransferase inhibitor, on, Propionibacterium acnes and lipopolysaccharide-induced hepatitis in mice. Eur J Pharmacol. 2007 Mar 8;558(1-3):179-84.

[4]. M T HOEKENGA. The treatment of acute malaria with single oral doses of amodiaquin, chloroquine, hydroxychloroquine and pyrimethamine. Am J Trop Med Hyg. 1954 Sep;3(5):833-8.

盐酸阿莫地喹物理化学性质

[ 沸点 ]:
478ºC at 760 mmHg

[ 分子式 ]:
C₂₀H₂₃Cl₂N₃O

[ 分子量 ]:
392.322

[ 精确质量 ]:
391.121826

[ PSA ]:
48.39000

[ LogP ]:
6.05420

[ 外观性状 ]:
粉末

[ 储存条件 ]:
-20℃

盐酸阿莫地喹毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: GO7300100

CHEMICAL NAME :: o-Cresol, 4-((7-chloro-4-quinolyl)amino)-alpha-(diethylamino)-, dihydrochloride

CAS REGISTRY NUMBER :: 69-44-3

LAST UPDATED :: 199707

DATA ITEMS CITED :: 2

MOLECULAR FORMULA :: C20-H22-Cl-N3-O.2Cl-H

MOLECULAR WEIGHT :: 428.82

WISWESSER LINE NOTATION :: T66 BNJ IG EMR DQ C1N2&2 &GH 2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 52 mg/kg/13W-I

TOXIC EFFECTS :: Blood - agranulocytosis

REFERENCE :: BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 292,717,1986

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 137 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 24,1471,1981

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盐酸阿莫地喹安全信息

[ 危害码 (欧洲) ]:
N

[ 海关编码 ]:
2933499090

盐酸阿莫地喹海关

[ 海关编码 ]: 2933499090

[ 中文概述 ]:
2933499090. 其他含喹琳或异喹啉环系的化合物〔但未进一步稠合的〕. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933499090. other compounds containing in the structure a quinoline or isoquinoline ring-system (whether or not hydrogenated), not further fused. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%