Article
Anticholinergic antiparkinson drug orphenadrine inhibits HERG channels: block attenuation by mutations of the pore residues Y652 or F656.
Naunyn-Schmiedeberg's archives of pharmacology - 1 Dec 2007
Scholz Eberhard P, Konrad Franziska M, Weiss Daniel L, Zitron Edgar, Kiesecker Claudia, Bloehs Ramona, Kulzer Martin, Thomas Dierk, Kathöfer Sven, Bauer Alexander, Maurer Martin H, Seemann Gunnar, Katus Hugo A, Karle Christoph A
Abstract excerpt
The anticholinergic antiparkinson drug orphenadrine is an antagonist at central and peripheral muscarinic receptors. Orphenadrine intake has recently been linked to QT prolongation and Torsade-de-Pointes tachycardia. So far, inhibitory effects on I (Kr) or cloned HERG channels have not been examined. HERG channels were heterologously expressed in a HEK 293 cell line and in Xenopus oocytes and HERG current was...
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