The voltage-dependent potassium channel hERG (human Ether-a-gogo Related Gene) plays a key role in the repolarization of the cardiac action potential (QT interval). Its inhibition can lead to potentially lethal cardiac arrhythmias.
Characterizing the absence of interaction with the hERG channel is an essential prerequisite for the development of molecules for therapeutic use.
The proposed test is based on the equilibrium binding technique of a radioactive antagonist ligand of the hERG channel, [3H]-Dofetilide. It allows the evaluation of the binding inhibition properties of this radioligand by molecules provided by the client, or the pharmacological properties of hERG samples provided by the client.
To be adapted according to the test
| Format | 96 wells | ||
| Biological sample | total membrane preparations (recombinant hERG) | ||
| hERG incubation in the presence of [3H]-Dofetilide, with or without competing ligand (control ligand Astemizole and/or compounds to be tested) | |||
| Fast filtration on harvester | |||
| Addition of sparkling cocktail and scintillation counting (TopCount PE) | |||
