Table 2.
Representative transport substrates for ATP-Binding Cassette (ABC) and Solute Carrier (SLC) transporters at the Blood-Brain Barrier (BBB).
Transporter | Representative Centrally Active Transport Substrates |
---|---|
OATPs/Oatps
(SLCOs/Slcos) |
HMG CoA Reductase Inhibitors (i.e., statins; atorvastatin, pravastatin, rosuvastatin) [5,96] Prostaglandin E2 [96] Estrone-3-Sulfate, Dihydroepiandrosterone Sulfate (DHEAS), Estradiol-17β-Glucuronide [97] |
OCTs/Octs
(SLC22A/Slc22a) |
Memantine [5] Pramipexole, Selegiline, Varenicline [6] Amisulpride [98] Metformin [99] |
MATE1/Mate1
(SLC47A1/Slc47a1) |
Metformin, Thiamine, Topotecan [96] Amisulpride [98] |
P-gp (MDR1/Mdr1)
(ABCB1/Abcb1a/Abcb1b) |
Amitriptyline, Cyclosporine A, Lapatinib, Losartan, Lovastatin, Phenytoin, Tetracycline, Verapamil [96] Atorvastatin, Rosuvastatin [100] Tacrolimus, Rifampicin [29] |
BCRP/Bcrp
(ABCG2/Abcg2) |
Coumestrol, Daidzein, Dantrolene, Dipyridamole, Estradiol-17β-Glucuronide, Genistein, Glyburide, Lapatinib [96] Atorvastatin, Pravastatin, Rosuvastatin [100] Estrone-3-Sulfate, Dihydroepiandrosterone Sulfate (DHEAS), Dihydrotestosterone (DHT) [97] |
MRPs/Mrps
(ABCC/Abcc) |
Glutathione (GSH), GSH Conjugates, GSSG [5] Estradiol-17β-Glucuronide [96] Estrone-3-Sulfate, Dihydroepiandrosterone Sulfate (DHEAS) [97] |