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

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Colabufo NA, Berardi F, Contino M, Inglese C, Niso M, Perrone R

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.

PubMed ID

18524592 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Cyclosporine	P-glycoprotein 1	EC 50 (nM)	45500	N/A	N/A	Details
Tamoxifen	P-glycoprotein 1	EC 50 (nM)	56500	N/A	N/A	Details
Verapamil	P-glycoprotein 1	EC 50 (nM)	20000	N/A	N/A	Details