Naringin directly activates inwardly rectifying potassium channels at an overlapping binding site to tertiapin-Q.

ABSTRACT:

Background

G protein-coupled inwardly rectifying potassium (K(IR) 3) channels are important proteins that regulate numerous physiological processes including excitatory responses in the CNS and the control of heart rate. Flavonoids have been shown to have significant health benefits and are a diverse source of compounds for identifying agents with novel mechanisms of action.

Experimental approach

The flavonoid glycoside, naringin, was evaluated on recombinant human K(IR) 3.1-3.4 and K(IR) 3.1-3.2 expressed in Xenopus oocytes using two-electrode voltage clamp methods. In addition, we evaluated the activity of naringin alone and in the presence of the K(IR) 3 channel blocker tertiapin-Q (0.5 nM, 1 nM and 3 nM) at recombinant K(IR) 3.1-3.4 channels. Site-directed mutagenesis wa

SUBMITTER: Yow TT 

PROVIDER: S-EPMC3130948 | biostudies-literature | 2011 Jul

REPOSITORIES: biostudies-literature