TABLE 1

Major drug transporters expressed in intestine, kidney, liver, and brain of human or rat

Human Rat
Name Localization Name Localization
Intestine
    Peptide transporter
         PEPT1 BBM PepT1 BBM
    Organic anion transporter
         OATP-B NDa Oatp3 BBM
         OATP-D ND
         OATP-E ND
         ASBT BBM Asbt BBM
    Organic cation transporter
Oct1 BLM
Oct3 ND
Octn1 ND
    Primary active transporter
         MDR1 BBM Mdr1 BBM
         MRP2 BBM Mrp2 BBM
         MRP3 BLM Mrp3 BLM
         BCRP BBM
Kidney
    Peptide transporter
PepT1 BBM
         PEPT2 ND PepT2 BBM
    Organic anion transporter
         OAT1 BLM Oat1 BLM
         OAT3 BLM Oat3 BLM
         OAT4 BBM
Oatp1 BBM
Oat-K1 BBM
Oat-K1 ND
NaPi-1/Npt1 BBM
Asbt BBM
    Organic cation transporter
Oct1 BLM
Oct1A ND
         OCT2 BLM Oct2 BLM
Oct3 ND
         OCTN1 ND Octn1 BBM
         OCTN2 ND Octn2 BBM
    Primary active transporter
         MDR1 BBM Mdr1 BBM
         MRP2 BBM Mrp2 BBM
         MRP4 BBM Mrp4 BBM
Liver
    Organic anion transporter
         NTCP SM Ntcp SM
         OATP-C SM Oatp1 SM
         OATP8 SM Oatp2 SM
         OATP-B SM Oatp4 SM
         OAT2 SM Oat2 SM
Oat3 SM
NaPi-1/Npt1 SM
    Organic cation transporter
         OCT1 ND Oct1 SM
Oct1A ND
         OCT3
Octn1 ND
    Primary active transporter
         MRP1 SM
         MRP3 SM Mrp3 (EHBR, TR-) SM
         MDR1 CM Mdr1 CM
         MRP2 CM Mrp2 CM
         BSEP/SPGP CM Bsep/Spgp CM
         BCRP CM
Brain capillary endothelial cells
    Organic anion transporter
         OATP-A ND Oat2 ALM, LM
Oat3 ND
    Organic cation transporter
Oct2 ND
    Primary active transporter
         MDR1 LM Mdr1 LM
Mrp1 ND
Mrp5 ND
Choroid plexus
    Peptide transporter
PepT2 BBM
    Organic anion transporter
Oatp1 BBM
Oatp2 BLM
Oatp3 BBM
    Primary active transporter
Oat3 BBM
Mrp1 BLM
Mdr1 BBM
  • SM, sinusoidal membrane; CM, canalicular membrane; BLM, basolateral membrane; BBM, brush border membrane; LM, luminal membrane, ALM, abluminal membrane.

  • a ND, not determined.