Transport of Bupropion and its Metabolites by the Model CHO and HEK293 Cell Lines.

ABSTRACT:

Background

Bupropion (BUP) is widely used as an antidepressant and smoking cessation aid. There are three major pharmacologically active metabolites of BUP, Erythrohydrobupropion (EB), Hydroxybupropion (OHB) and Threohydrobupropion (TB). At present, the mechanisms underlying the overall disposition and systemic clearance of BUP and its metabolites have not been well understood, and the role of transporters has not been studied.

Objective

The goal of this study was to investigate whether BUP and its active metabolites are substrates of the major hepatic uptake and efflux transporters.

Method

CHO or HEK293 cell lines or plasma membrane vesicles that overexpress OATP1B1, OATP1B3, OATP2B1, OATP4A1, OCT1, BCRP, MRP2 or P-gp were used in cellular or vesicle uptake and inhib

SUBMITTER: Han LW 

PROVIDER: S-EPMC7451048 | biostudies-literature | 2019

REPOSITORIES: biostudies-literature