Amodiaquine 2HCl Dihydrate

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Chemical Structure| 6398-98-7 同义名 : 阿莫地喹盐酸盐 ;Amodiaquin dihydrochloride dihydrate; Amodiaquine dihydrochloride dihydrate
CAS号 : 6398-98-7
货号 : A109447
分子式 : C20H28Cl3N3O3
纯度 : 97%
分子量 : 464.81
MDL号 : MFCD09260307
存储条件：

Pure form Inert atmosphere, room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 Amodiaquin Dihydrochloride Dihydrate is a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor[3]. 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[4]. 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[5].The administration of amodiaquine (2 mg/kg, 5 mg/kg, s.c.) partially improved the survival rate of the C57BL/6 mice, Amodiaquine (2 mg/kg) decreased the LPS-induced increase in serum ALT levels at 6 h and AST levels at 6 h, whereas amodiaquine (5 mg/kg) decreased the LPS-induced increase in serum ALT levels at 3 h and 6 h and AST levels at 6 h. Amodiaquine dose-dependently lowered TNF-α levels in comparison to the saline treated mice, and abolished the increase in TNF-α mRNA in liver of P. acnes-primed and LPS-treated mice[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.15mL

0.43mL

0.22mL

10.76mL

2.15mL

1.08mL

21.51mL

4.30mL

2.15mL
参考文献

[1]Yokoyama A, Mori S, 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.

[2]Horton JR, Sawada K, et al. Structural basis for inhibition of histamine N-methyltransferase by diverse drugs. J Mol Biol. 2005 Oct 21;353(2):334-344.

[3]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.

[4]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.

[5] 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.

[6]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.