amodiaquine-free-base

Description: Amodiaquin (trade names Camoquin, Flavoquine) is a potent and orally bioactive inhibitor of the Ebola virus, acts by targeting the viral protein 35 (VP35). It is also a 4-aminoquinoline class of antimalarial agent and anti-inflammatory agent that inhibits histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ca.20 uM. Amodiaquine has been shown to be more effective than chloroquine in treating chloroquine-resistant Plasmodium falciparum malaria infections and may give more protection than chloroquine when used as weekly prophylaxis. Amodiaquine, like chloroquine, is generally well tolerated. Amodiaquine is a histamine N-methyltransferase inhibitor. It is on the World Health Organization's List of Essential Medicines, the most important medications needed in a basic health system.

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. Dhiman V, Singh DK, Ladumor MK, Singh S. Characterization of stress degradation products of amodiaquine dihydrochloride by liquid chromatography with high-resolution mass spectrometry and prediction of their properties by using ADMET Predictor. J Sep Sci. 2017 Dec; 40(23):4530-4540. doi: 10.1002/jssc.201700904. Epub 2017 Oct 30. PubMed PMID: 28985017.

Related CAS #: 86-42-0 (free base) 69-44-3 (HCl) 6398-98-7 (HCl hydrate)