Functional identification of organic cation transporter 1 as an atenolol transporter sensitive to flavonoids.

ABSTRACT: Atenolol, a β1-adrenergic receptor blocker, is administered orally and its intestinal absorption has recently been indicated to be mediated by carrier protein and reduced markedly by ingestion of some fruit juices, such as apple and orange juices. This could be postulated to be a problem arising from the interaction of some components of fruit juices with atenolol at a transporter involved in its intestinal uptake, but the responsible transporter and its interacting components have not been identified yet. In an attempt to examine that possibility, we could successfully find that human organic cation transporter 1 (OCT1/SLC22A1), which is suggested to be expressed at the brush border membrane of enterocytes, is highly capable of transporting atenolol. In this attempt, OCT1 was stably expre

SUBMITTER: Mimura Y 

PROVIDER: S-EPMC5668658 | biostudies-literature | 2015 Jul

REPOSITORIES: biostudies-literature