Rat in vivo liver studies including functional testing of ratMrp2, ratBsep and ratBcrp transporters In vivo biliary efflux experiments are performed on male Wistar rats kept under standard laboratory conditions.
All procedures are approved by the Institutional Animal Care and Use Committee. Tracer doses of 3H-Estradiol-17-b-D-glucuronide, 3H-Taurocholate, 3H-Estrone-3-sulfate, probe substrates for Mrp2, Bsep and Bcrp, respectively are co-administered with the test compounds i.p. Control rats receive the probe substrates and the vehicle only. Bile samples are collected, weighted and analyzed by liquid scintillation. Interactions with the transport proteins are determined from the altered biliary elimination of the probe substrates.
A representation of the assay is shown in Figure 1.
Figure 1. Inhibition of taurocholate transport of ratBsep transporters by cyclosporin
A in in vivo experiments Click here for more information on hepatic efflux and uptake transporters.