Desmethylastemizole (O-Demethylastemizole) , a metabolite of Astemizole ( HY-12532 ), is a β-hematin (βH) inhibitor. Desmethylastemizole has an antiplasmodium activity against P. falciparum with IC 50 of 0.12, 0.11 and 0.06 μM for Pf 3D7, Pf Dd2, and Pf ItG strains, respectively. Desmethylastemizole is also a Histamine H1 receptor antagonist. Desmethylastemizole significantly blocks hERG K + channels and also inhibits histone-lysine N-methyltransferase EZH2 activity. Desmethylastemizole can be used for long QT syndrome and malaria research.
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