Bcrp Knockout Rat
Model Detail >
- Efflux assay
- Blood brain barrier efflux
- Drug-drug interactions
- Tissue distribution
- Efficacy assay
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BCRP plays a protective role in neurotoxicity by limiting the efflux of xenobiotics into the brain. Homozygous null rats demonstrate increased exposure in the brain and plasma when dosed with BCRP-specific substrates.
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- Biallelic 588 bp deletion within Abcg2 gene
- Homozygous knockouts display total loss of protein via Western blot
- Increased oral bioavailability of BCRP-specific substrates
- Sprague-Dawley background strain
Figure 1. Oral absorption of sulfasalazine
Figure 2. Dantrolene level of Bcrp (-/-) and wild type rats 2 hours after treatment (nM/g)
Loss of function of Bcrp leads to improper transport of drugs across epithelial cells and increased bioavailability of Bcrp substrates. This model is useful for studying metabolism of xenobiotic compounds, tissue distribution, DMPK, efficacy, formulation, and blood brain barrier efflux.
- Zamek-Gliszczynski, M, et al. Minor compensatory changes in SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats do not detract from their utility in the study of transporter-mediated pharmacokinetics.
- Zamek-Gliszczynski, M, et al. Characterization of SAGE Labs Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics. DMD. 2012