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. Author manuscript; available in PMC: 2012 Feb 1.
Published in final edited form as: Drug Metab Rev. 2010 Sep 21;43(1):27–40. doi: 10.3109/03602532.2010.512294

Table 3.

Drug transporter genetically modified mouse models.

Gene Category Example applications References
Mdr1a (Abcb1a) Knockout Drug absorption, distribution and elimination, including brain penetration (Schinkel et al., 1994; Schinkel et al., 1995; Schinkel et al., 1996)
Mdr1a/1b (Abcb1a/1b) Knockout Drug distribution (Schinkel et al., 1997)
Bsep (Abcb11) Knockout Bile acid distribution and excretion (Wang et al., 2001; Wang et al., 2003)
Mrp1 (Abcc1) Knockout Disposition of xenobiotic drugs and endogenous leukotrienes (Wijnholds et al., 1997)
(Lorico et al., 1997)
Mrp2 (Abcc2) Knockout Glutathione excretion, bile flow and drug disposition (Vlaming et al., 2006)
(Chu et al., 2006)
Mrp3 (Abcc3) Knockout Acetaminophen disposition; biliary excretion (Belinsky et al., 2005)
(Zelcer et al., 2006)
Mrp4 (Abcc4) Knockout Drug resistance and brain penetration. (Leggas et al., 2004)
Bcrp1 (Abcg2) Knockout Drug absorption, distribution and elimination, including the secretion of compounds into milk (Zhou et al., 2002)
(Jonker et al., 2002)
Ostα Knockout Bile acid disposition (Rao et al., 2008)
Pept2 (Slc15a2) Knockout Role of Pept2 in drug distribution and excretion (Rubio-Aliaga et al., 2003)
(Shen et al., 2003; Shen et al., 2007)
Mate1 (Slc47a1) Knockout Renal secretion of metformin (Tsuda et al., 2009)
Oct1 (Slc22a1) Knockout Hepatic uptake and intestinal disposition of organic cation drugs (Jonker et al., 2001)
Oct2 (Slc22a2)
Oct1/2 (Slc22a1/2)
Knockout Renal excretion of drugs (Jonker et al., 2003)
Oct3 (Slc22a3) Knockout Role of Oct3 in drug distribution (Zwart et al., 2001)
Oat1 (Slc22a6) Knockout Excretion of organic anions and drugs (Eraly et al., 2006)
Oat3 (Slc22a8) Knockout Uptake of organic anions and drugs (Sweet et al., 2002) (Sykes et al., 2004)
OATP1B1 (SLCO1B1) Transgenic Hepatic uptake of mitoxantrone (van de Steeg et al., 2009)
Oatp1b2 (Slco1b2) Knockout Drug disposition and hepatic uptake (Zaher et al., 2008) (Lu et al., 2008) (Chen et al., 2008)