Affinity-assay for the human erg potassium channel

Details Affinity-assay for the human erg potassium channel Affinity-assay for the human erg potassium channel

G - Physics

01

N

G01N 33/566 (2006.01) G01N 33/50 (2006.01) G01N 33/68 (2006.01)

Patent

CA 2459265

The invention relates to an assay to establish the affinity of compounds at the "ether-a-go-go" (ERG) potassium (K+) channel, in particular the human ERG (hERG) potassium channel, using a labelled inwardly rectifying potassium channel (IKR) blocker. This assay is useful to identify compounds with undesirable effects on cardiac repolarisation in man, in particular the propensity to prolong the QT interval in the electrocardiogram.

L'invention concerne un dosage permettant de déterminer l'affinité de composés pour le canal potassique (K<+>) "éther-à-go-go" (ERG), en particulier le canal potassique ERG humain (hERG), au moyen d'un bloqueur de canal potassique à rectification entrante (KIR) marqué. Le dosage selon l'invention est utilisé pour identifier des composés présentant des effets indésirables sur la repolarisation cardiaque chez un homme et, en particulier, une propension à prolonger l'intervalle QT de l'électrocardiogramme.

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