Table 2.
Ligands | SLC | EPA | Caco-2 | VB-Caco-2 | MDCK | MDCK-MDR1 | |||||
---|---|---|---|---|---|---|---|---|---|---|---|
Papp A-B | PDR | Papp A-B | PDR | Papp A-B | PDR | Papp A-B | PDR | Papp A-B | PDR | ||
Glucopyranose | GLUT1 | <65.7 | >0.14 | 57.83 | 0.64 | 17.17 | 1.17 | <18.5 | NA | <18.5 | NA |
Valproic acid | LAT1, OATPs | 39.37 | 0.98 | 51.91 | 0.82 | 42.22 | 0.87 | 26.62 | 1.22 | 27.49 | 1.26 |
Baclofen | LAT1 | 16.34 | 0.85 | 1.23 | 0.77 | 0.31 | 0.47 | 1.28 | 0.77 | 0.68 | 0.82 |
Gabapentin | LAT1, Pgp, BCRP | 2.98 | 0.92 | 1.80 | 0.77 | <0.88 | >0.27 | 3.35 | 0.28 | 4.75 | 0.42 |
Probenecid | MCT, OATs | 18.96 | 0.79 | 27.34 | 0.88 | 33.39 | 0.88 | 19.37 | 0.83 | 17.23 | 0.98 |
Salicylic acid | MCT1, OATPs, MRP4 | 4.78 | 1.88 | 16.63 | 1.11 | 7.60 | 1.19 | 13.01 | 0.86 | 9.31 | 0.85 |
Rosuvastatin | OATPs, Pgp, MRP2, BCRP | 11.31 | 0.80 | 0.92 | 9.41 | 0.38 | 12.80 | 0,.9 | 0.52 | 0.81 | 1.13 |
Pravastatin | OATPs, MRP2 | 7.61 | 1.14 | 1.50 | 0.90 | 0.19 | 0.80 | 0.58 | 2.40 | 0.30 | 1.09 |
Atorvastatin | OATPs, MCT, Pgp, MRP2, BCRP | 3.93 | 1.44 | 7.53 | 1.28 | 2.98 | 4.34 | 2.36 | 1.09 | 1.66 | 5.76 |
BCRP, breast cancer resistance protein; GLUT1, glucose transporters; LAT1, large neutral amino acid transporter; MCT, monocarboxylic acid transporter; MRP, multidrug resistance-associated proteins; OAT, organic anion transporter; OATP, organic anion-transporting polypeptide; PDR, permeability directional ratio; Pgp, P glycoprotein.