Title : Mechanism of block of hEag1 K+ channels by imipramine and astemizole.

Pub. Date : 2004 Oct

PMID : 15365094






3 Functional Relationships(s)
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1 Mechanism of block of hEag1 K+ channels by imipramine and astemizole. Imipramine potassium voltage-gated channel subfamily H member 1 Homo sapiens
2 The tricyclic antidepressant imipramine and the antihistamine astemizole inhibit the current through Eag1 channels and reduce the proliferation of cancer cells. Imipramine potassium voltage-gated channel subfamily H member 1 Homo sapiens
3 Even if both drugs differ in their affinity for hEag1 channels (IC50s are approximately 2 microM for imipramine and approximately 200 nM for astemizole) and in their blocking kinetics, both drugs permeate the membrane and inhibit the hEag1 current by selectively binding to open channels. Imipramine potassium voltage-gated channel subfamily H member 1 Homo sapiens