Effect of some P-glycoprotein modulators on Rhodamine-123 absorption in guinea-pig ileum.
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.
Colabufo
Nicola Antonio
NA
Dipartimento Farmacochimico, Università degli Studi di Bari, via Orabona, 4, 70125 Bari, Italy. colabufo@farmchim.uniba.it
Berardi
Francesco
F
Contino
Marialessandra
M
Inglese
Carmela
C
Niso
Mauro
M
Perrone
Roberto
R
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000737:chemistry*; D000818:Animals; D018938:Caco-2 Cells; D002626:Chemistry, Pharmaceutical / Q000379:methods; D016572:Cyclosporine / Q000494:pharmacology; D051544:Cytochrome P-450 CYP3A / Q000737:chemistry; D003577:Cytochrome P-450 Enzyme System / Q000737:chemistry; D018432:Drug Resistance, Multiple; D006168:Guinea Pigs; D006801:Humans; D007082:Ileum / Q000187:drug effects* / Q000378:metabolism; D008956:Models, Chemical; D020112:Rhodamine 123 / Q000737:chemistry* / Q000493:pharmacokinetics*; D013629:Tamoxifen / Q000494:pharmacology; D014700:Verapamil / Q000494:pharmacology
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D013629:Tamoxifen; D020112:Rhodamine 123; D016572:Cyclosporine; D003577:Cytochrome P-450 Enzyme System; D014700:Verapamil; D051544:Cytochrome P-450 CYP3A; C510163:CYP3A4 protein, human