Efflux Inhibition Experiments Using CACO-2 Cells

Schwab D, Fischer H, Tabatabaei A, Poll S, Huwyler J (2003) Comparison of in vitro P-glycoprotein screening assays recommendations for their use in drug discovery. J Med Chem 46(9) 1716—1725 

Takara K, Tsujimoto M, Ohnishi N et al. (2003) Effects of continuous exposure to digoxin on MDR1 function and expression in CACO.2 cells. J Pharm Pharmacol 55 675-681 Taipalensuu J, Tornblom H, Lindberg G et al. (2001) Correlation of gene expression of ten drug efflux proteins of the ATP- binding cassette transporter family in normal human jejunum and in human intestinal CACO-2 cell monolayers. J Pharmacol Exp Ther 299 164-170 

Examples of efflux studies using CACO-2 and other cells expressing efflux transporters are given in the studies of Schwab et al. (2003), Polli et al. (2001), Pachot et al. (2003) and others. 

Efflux Inhibition Experiments Using CACO-2 Cells 

PURPOSE AND RATIONALE Once a compound is identified in an efflux assays it is sometimes of importance to discriminate between efflux, inhibition potential and to determine the efflux transporter responsible for efflux of the compound. 

---

II.D.5 Efflux Inhibition Experiments Using CACO-2 Cells... 

---