Screening for potassium channel modulators by a high through-put 86-rubidium efflux assay in a 96-well microtiter plate.

A rapid and sensitive 86Rb efflux assay to detect chemical compounds capable of modulating the ATP-dependent potassium (KATP) channel is described. This assay, which is performed in a 96-well microtiter plate, utilizes a substrate adherent cell line as the target, requires a small amount of 86Rb as the tracer, and is a suitable system for performing the biochemical and pharmacological characterization of the KATP-channel and its activators. Because this assay is amenable to automation, it presents a useful means for high-volume screening of chemical compounds on a routine basis.