Effect of some P-glycoprotein modulators on Rhodamine-123 absorption in guinea-pig ileum

Nicola Antonio Colabufo; Francesco Berardi; Marialessandra Contino; Carmela Inglese; Mauro Niso; Roberto Perrone

doi:10.1016/j.bmcl.2008.05.055

Effect of some P-glycoprotein modulators on Rhodamine-123 absorption in guinea-pig ileum

Bioorg Med Chem Lett. 2008 Jul 1;18(13):3741-4. doi: 10.1016/j.bmcl.2008.05.055. Epub 2008 May 20.

Authors

Nicola Antonio Colabufo¹, Francesco Berardi, Marialessandra Contino, Carmela Inglese, Mauro Niso, Roberto Perrone

Affiliation

¹ Dipartimento Farmacochimico, Università degli Studi di Bari, via Orabona, 4, 70125 Bari, Italy. colabufo@farmchim.uniba.it

PMID: 18524592
DOI: 10.1016/j.bmcl.2008.05.055

Abstract

Several reference compounds such as Cyclosporin A, Tamoxifen, Verapamil, and our compound 1, known as P-gp modulators, have been tested for their P-gp modulating activity in isolated organ bath. Compound 1 showed the best result in organ bath experiment (EC(50)=14.7 microM), Cyclosporin A and Tamoxifen displayed EC(50)=25.2 and 39.4 microM, respectively.

MeSH terms

ATP Binding Cassette Transporter, Subfamily B, Member 1 / chemistry*
Animals
Caco-2 Cells
Chemistry, Pharmaceutical / methods
Cyclosporine / pharmacology
Cytochrome P-450 CYP3A / chemistry
Cytochrome P-450 Enzyme System / chemistry
Drug Resistance, Multiple
Guinea Pigs
Humans
Ileum / drug effects*
Ileum / metabolism
Models, Chemical
Rhodamine 123 / chemistry*
Rhodamine 123 / pharmacokinetics*
Tamoxifen / pharmacology
Verapamil / pharmacology

Substances

ATP Binding Cassette Transporter, Subfamily B, Member 1
Tamoxifen
Rhodamine 123
Cyclosporine
Cytochrome P-450 Enzyme System
Verapamil
Cytochrome P-450 CYP3A
CYP3A4 protein, human