Finding Inward Rectifier Channel Inhibitors: Why and How?

Marcel A G Van Der Heyden

doi:10.3389/fphar.2011.00095

Abstract

GENERAL COMMENTARY article Front. Pharmacol., 09 January 2012Sec. Pharmacology of Ion Channels and Channelopathies volume 2 - 2011 | https://doi.org/10.3389/fphar.2011.00095

Highlights

Standard single cell patch clamp methods allow highly detailed characterization of the inhibiting capacity and its underlying mechanisms of new compounds for virtually every ion channel of interest, including Kir channels
Upon stimulation of channel opening, thallium from the bath medium enters the cell through Kir channels, resulting in increased fluorescence
New lead compounds for every Kir class will likely be derived from screening efforts of public, academic, or private owned compound libraries (e.g., Wang et al, 2011), or from development of existing drugs displaying Kir channel block as an apparent side effect (Van der Heyden and Sánchez-Chapula, 2011)

Summary

Introduction

Standard single cell patch clamp methods allow highly detailed characterization of the inhibiting capacity and its underlying mechanisms of new compounds for virtually every ion channel of interest, including Kir channels. The last decade, a number of non-electrophysiological Kir assay systems have been developed that allow large scale screening assays . The latter makes use of a thallium sensitive fluorescent probe loaded into Kir expressing cells.

Results

Conclusion