Astemizole is a non-sedating antihistamine that antagonizes the histamine H1 receptor with a Ki value of 4.4 nM.{25629} It is considerably less potent at muscarinic acetylcholine receptors (Ki = 2.4 ?M).{23214} Astemizole is also a potent blocker of ether-a-go-go-related gene (ERG) potassium channels (IC50 = ~1 nM) that has been used to study long QT syndrome type 2.{24505,24504} Furthermore, because it can target oncogenic ERG1 and ERG potassium channels, astemizole has been explored as a potential antineoplastic agent for decreasing proliferation of various cancer cells.{27578}
产品描述
A histamine H1 receptor antagonist (Ki = 4.4 nM) that also blocks ERG potassium channels (IC50 = ~1 nM); used to study long QT syndrome type 2 and as an antineoplastic agent for decreasing proliferation of various cancer cells
