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 (EC50 = 14.7 μM), Cyclosporin A and Tamoxifen displayed EC50 = 25.2 and 39.4 μM, respectively.

The inhibition of Rhodamine-123 efflux in guinea-pig ileum by several P-gp inhibitors is reported.Figure optionsDownload as PowerPoint slide