Trapping and dissociation of propafenone derivatives in HERG channels.

ABSTRACT:

Background and purpose

Human ether-a-go-go related gene (HERG) channel inhibitors may be subdivided into compounds that are trapped in the closed channel conformation and others that dissociate at rest. The structural peculiarities promoting resting state dissociation from HERG channels are currently unknown. A small molecule-like propafenone is efficiently trapped in the closed HERG channel conformation. The aim of this study was to identify structural moieties that would promote dissociation of propafenone derivatives.

Experimental approach

Human ether-a-go-go related gene channels were heterologously expressed in Xenopus oocytes and potassium currents were recorded using the two-microelectrode voltage clamp technique. Recovery from block by 10 propafenone derivatives with

SUBMITTER: Windisch A 

PROVIDER: S-EPMC3057292 | biostudies-literature | 2011 Apr

REPOSITORIES: biostudies-literature