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[CAS NO. 69-44-3] Amodiaquine dihydrochloride
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| Catalog: | HY-B1322B |
| Brand: | MCE |
| CAS: | 69-44-3 |
Overview
| MDL | MFCD00078857 |
|---|---|
| Molecular Weight | 428.78 |
| Molecular Formula | C20H24Cl3N3O |
| SMILES | [H]Cl.[H]Cl.OC1=CC=C(NC2=CC=NC3=CC(Cl)=CC=C23)C=C1CN(CC)CC |
6 Publications Citing Use of MCE
Summary
Amodiaquine dihydrochloride (Amodiaquin dihydrochloride), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor with a K i of 18.6 nM. Amodiaquine dihydrochloride is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC 50 of ~20 μM. Anti-inflammatory effect [1] [2] [3] [4] [5] .
IC50 & Target
In Vitro
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
[1]
.
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
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
RT-PCR [1]
| 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. |
In Vivo
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 [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male ICR mice (8-10 weeks of age) induced ntracerebral hemorrhage (ICH) [2] |
| Dosage: | 40 mg/kg |
| Administration: | Intraperitoneal injection; daily; for 3 days |
| Result: | Diminished perihematomal activation of microglia/macrophages and astrocytes. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00146718 | London School of Hygiene and Tropical Medicine|University of Yaounde |
Malaria
|
August 2003 | Phase 2|Phase 3 |
| NCT00164359 | Centers for Disease Control and Prevention|Ministry of Health and Population, Malawi |
Malaria, Falciparum
|
April 2005 | Phase 4 |
| NCT00852371 | London School of Hygiene and Tropical Medicine|Uganda Malaria Surveillance Project|Ministry of Health, Uganda |
Malaria|Intermittent Preventive Treatment
|
February 2008 | Phase 3 |
| NCT04149106 | University Clinical Research Center, Mali|Tulane University|University of South Florida|University of Copenhagen|Deakin University|Johns Hopkins University |
Malaria,Falciparum
|
July 1, 2019 | Phase 1 |
| NCT03923725 | University of Oxford|Mahidol Oxford Tropical Medicine Research Unit |
Plasmodium Falciparum Malaria (Uncomplicated)
|
September 1, 2020 | Phase 3 |
| NCT01955382 | National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health Clinical Center (CC) |
Malaria|Severe Malaria
|
September 2013 | Phase 2 |
| NCT03431714 | National Institute for Medical Research, Tanzania|Muhimbili University of Health and Allied Sciences|World Health Organization |
Uncomplicated Falciparum Malaria
|
July 14, 2017 | Phase 4 |
| NCT00356824 | National Institute of Allergy and Infectious Diseases (NIAID) |
HIV Infections|Malaria
|
November 2005 | |
| NCT02211729 | London School of Hygiene and Tropical Medicine|Malaria Research and Training Center, Bamako, Mali|Institut de Recherche en Sciences de la Sante, Burkina Faso |
Malaria|Respiratory Infections
|
May 2014 | Phase 3 |
| NCT00386503 | Sanofi |
Malaria
|
June 2006 | Phase 1 |
| NCT00894660 | Pfizer |
Falciparum Malaria
|
June 2009 | Phase 1 |
| NCT00529620 | London School of Hygiene and Tropical Medicine|Cheikh Anta Diop University, Senegal |
Malaria
|
September 2007 | Phase 3 |
| NCT00146731 | London School of Hygiene and Tropical Medicine|National Institute for Medical Research, Tanzania |
Malaria
|
January 2004 | Phase 3 |
| NCT04816461 | Institut de Recherche en Sciences de la Sante, Burkina Faso |
Malaria
|
July 2021 | Phase 4 |
| NCT00111163 | Centers for Disease Control and Prevention|Kenya Medical Research Institute|Bill and Melinda Gates Foundation |
Malaria|Anemia
|
March 2004 | Not Applicable |
| NCT00137514 | Bandim Health Project |
Malaria, Falciparum
|
March 2001 | Phase 4 |
| NCT00712374 | London School of Hygiene and Tropical Medicine|Senegal: Ministere de la Sante|Institut de Recherche pour le Developpement|Cheikh Anta Diop University, Senegal |
Malaria
|
September 2008 | Phase 4 |
| NCT01378286 | Sanofi |
Malaria
|
January 2012 | Phase 3 |
| NCT00376155 | London School of Hygiene and Tropical Medicine|Medical Research Council |
Malaria
|
May 2006 | Phase 4 |
| NCT02696954 | University of Oxford|Mahidol University|Mahidol Oxford Tropical Medicine Research Unit |
Pharmacokinetic|Drug Combination|Healthy
|
November 18, 2016 | Phase 1|Phase 2 |
| NCT01152931 | University of Lagos, Nigeria |
Malaria
|
August 2010 | Phase 3 |
| NCT05471544 | Malaria Consortium |
Malaria
|
July 18, 2022 | Phase 3 |
| NCT00118807 | London School of Hygiene and Tropical Medicine|Medical Research Council|National Malaria Control Programme, The Gambia |
Malaria
|
August 2003 | Phase 3 |
| NCT01023399 | Sanofi|Medicines for Malaria Venture |
Malaria
|
November 2009 | Phase 4 |
| NCT00563914 | Sanofi |
Malaria
|
October 2007 | Phase 1|Phase 2 |
| NCT00316329 | Sanofi |
Malaria
|
March 2006 | Phase 3 |
| NCT01319448 | London School of Hygiene and Tropical Medicine|Medical Research Council Unit, The Gambia|Wellcome Trust|University of Ilorin Teaching Hospital |
Malaria|Sickle Cell Crisis
|
September 2011 | Phase 1|Phase 2 |
| NCT00354380 | Heidelberg University |
Malaria
|
September 2006 | Phase 2 |
| NCT00132548 | London School of Hygiene and Tropical Medicine|Institut de Recherche pour le Developpement, Senegal|Cheikh Anta Diop University, Senegal|Ministry of Health, Senegal |
Malaria
|
June 2004 | Phase 3 |
| NCT05478954 | Malaria Consortium |
Malaria
|
July 15, 2022 | Phase 4 |
| NCT00445796 | Sanofi |
Malaria
|
June 2005 | Phase 4 |
| NCT05354258 | London School of Hygiene and Tropical Medicine|Université de Thies, UFR Santé, Senegal |
Malaria|Soil Transmitted Helminths|Schistosomiasis|Integrated Control|Seasonal Malaria Chemoprevention|Mass Drug Administration With Anthelminthic Drugs
|
June 16, 2022 | Not Applicable |
| NCT00157885 | Menzies School of Health Research|National Institute of Health Research and Development, Ministry of Health Republic of Indonesia|Wellcome Trust|National Health and Medical Research Council, Australia |
Malaria, Falciparum|Malaria, Vivax
|
July 2005 | Not Applicable |
| NCT00323622 | GlaxoSmithKline |
Malaria
|
April 2005 | Phase 2 |
| NCT01328990 | London School of Hygiene and Tropical Medicine|Cheikh Anta Diop University, Senegal |
Malaria
|
April 2011 | Phase 1|Phase 2 |
| NCT00944840 | London School of Hygiene and Tropical Medicine |
Malaria
|
September 2008 | Phase 3 |
| NCT02831023 | University of California, San Francisco|Malaria Research and Training Center, Bamako, Mali|Radboud University Medical Center|London School of Hygiene and Tropical Medicine|Heidelberg University|Bill and Melinda Gates Foundation |
Malaria
|
July 2016 | Phase 2 |
| NCT05550909 | London School of Hygiene and Tropical Medicine |
Malaria,Falciparum
|
October 17, 2022 | Phase 2 |
| NCT03764527 | Professor Anders Björkman|Zanzibar Malaria Control Programme|World Health Organization|Karolinska Institutet |
Plasmodium Falciparum Malaria
|
November 1, 2002 | Phase 4 |
| NCT01651416 | Centre for Global Health Research, Ghana|London School of Hygiene and Tropical Medicine |
Malaria|Anaemia
|
July 2012 | Phase 4 |
| NCT05323721 | Malaria Consortium |
Malaria
|
June 1, 2022 | Phase 4 |
| NCT03768908 | Professor Anders Björkman|Zanzibar Malaria Control Programme|Karolinska Institutet |
Plasmodium Falciparum Malaria
|
January 5, 2005 | Phase 4 |
| NCT00550160 | Kwame Nkrumah University of Science and Technology|Department for International Development, United Kingdom|Malaria Consortium, UK|Center for International Health and Development |
Malaria
|
April 2007 | Phase 4 |
| NCT04080895 | University of Oxford|Mahidol University|Mahidol Oxford Tropical Medicine Research Unit |
Pharmacokinetic|Healthy|Drug Combination
|
November 1, 2022 | Phase 1 |
| NCT00465257 | Karolinska University Hospital |
Malaria
|
May 2007 | Phase 4 |
| NCT00127998 | Centers for Disease Control and Prevention|Malaria Research and Training Center, Bamako, Mali |
Malaria
|
July 2005 | Not Applicable |
| NCT05081089 | London School of Hygiene and Tropical Medicine |
Malaria,Falciparum
|
October 12, 2021 | Phase 2 |
| NCT00432367 | London School of Hygiene and Tropical Medicine|Kwame Nkrumah University of Science and Technology |
Malaria|Anaemia|Pregnancy
|
February 2007 | Phase 3 |
| NCT00261222 | Heidelberg University|Centre de Recherche en Sante de Nouna, Burkina Faso |
Malaria
|
September 2005 | Phase 2 |
| NCT00374205 | Bernhard Nocht Institute for Tropical Medicine|Presbyterian Health Service (PHS)|Kumasi Centre for Collaborative Research (KCCR)|School of Medical Sciences Kumasi (SMS+KNUST) |
Malaria, Falciparum
|
September 2006 | Phase 4 |
| NCT00131703 | London School of Hygiene and Tropical Medicine|Ministry of Health, Ghana |
Malaria|Pregnancy
|
March 2003 | Phase 3 |
| NCT00612547 | National Malaria Control Programme, Madagascar|Population Services International|Reggio Terzo Mondo|Santé Net|Inter Aide Santé,|Adventist Development and Relief Agency|SAF FJKM|Sanofi|Institut Pasteur de Madagascar |
Fever|Suspected Malaria
|
February 2008 | |
| NCT00146783 | London School of Hygiene and Tropical Medicine|Ministry of Health, Ghana |
Malaria
|
June 2004 | Phase 2|Phase 3 |
| NCT00164710 | Centers for Disease Control and Prevention|Ministry of Health and Population, Malawi |
Malaria, Falciparum
|
April 2005 | Phase 4 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : 125 mg/mL ( 291.52 mM ; Need ultrasonic)
H 2 O : 50 mg/mL ( 116.61 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.3322 mL | 11.6610 mL | 23.3220 mL |
| 5 mM | 0.4664 mL | 2.3322 mL | 4.6644 mL |
| 10 mM | 0.2332 mL | 1.1661 mL | 2.3322 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (4.85 mM); Clear solution
References
- [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.
- [5] John R Horton, et al. Structural basis for inhibition of histamine N-methyltransferase by diverse drugs. J Mol Biol. 2005 Oct 21;353(2):334-344.
Synonyms
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