Role of organic cation transporter 3 (SLC22A3) and its missense variants in the pharmacologic action of metformin.

ABSTRACT:

Objectives

The goals of this study were to determine the role of organic cation transporter 3 (OCT3) in the pharmacological action of metformin and to identify and functionally characterize genetic variants of OCT3 with respect to the uptake of metformin and monoamines.

Methods

For pharmacological studies, we evaluated metformin-induced activation of AMP-activated protein kinase, a molecular target of metformin. We used quantitative PCR and immunostaining to localize the transporter and isotopic uptake studies in cells transfected with OCT3 and its nonsynonymous genetic variants for functional analyses.

Results

Quantitative PCR and immunostaining showed that OCT3 was expressed high on the plasma membrane of skeletal muscle and liver, target tissues for metformin actio

SUBMITTER: Chen L 

PROVIDER: S-EPMC2976715 | biostudies-literature | 2010 Nov

REPOSITORIES: biostudies-literature