DRUG TRANSPORT IN THE LIVER - Drug Transporters: Molecular Characterization and Role in Drug Disposition - page 362

TABLE 13.1. Human Hepatic Uptake Transport Proteins
Protein/

Gene

Trivial Names Symbol Substrates/References

NTCP SLC10A1 BSP; cholate; estrone 3-sulfate; glycocholate;

taurochenodeoxycholate; tauroursodeoxycholate; TC
[280], Rosuvastatin [281]

OATP1A2
OATP-A
OATP-1
OATP

SLCO1A2
(SLC21A3)

Bile acids; BQ-123; BSP; DHEAS; DPDPE; E 2 17G; estrone
3-sulfate; n -methylquinine; ouabain; prostaglandin E 2 ;
T3; T4 [282], Deltorphin II [206,282], Fexofenadine
[139], Microcystin-LR [283], Saquinavir [284]

OATP1B1
OATP-C
LST-1
OATP2

SLCO1B1
(SLC21A6)

Atorvastatin [146,208], Benzylpenicillin [209], Bile acids;
BQ-123; BSP; DHEAS; DPDPE; E 2 17G; estrone
3-sulfate; T3; T4 [282], Bilirubin, bilirubin glucuronides
[285], LTC 4 ; prostaglandin E 2 [282,286], Caspofungin
[210], Cerivastatin [159,208], Fluvastatin [101],
Irinotecan metabolite (SN-38) [211], Methotrexate [286],
Microcystin-LR [283], Phalloidin (assessed by dimethyl
derivative) [212], Pitavastatin [213,214], Pravastatin
[208,215], Repaglinide [166,168], Rifampin [147,216],
Rosuvastatin [164,281], Simvastatin [208],
Troglitazone-sulfate [217]

OATP1B3
OATP-8
LST-2

SLCO1B3
(SLC21A8)

Bile acids; BQ-123; BSP; Deltorphin II; DHEAS; digoxin;
DPDPE; E 2 17G; estrone 3-sulfate; LTC 4 ; ouabain; T3; T4
[282], CCK-8 [218], Fexofenadine [219], Fluvastatin
[101], Microcystin-LR [283], Monoglucuronosyl bilirubin
[285], Paclitaxel [220], Phalloidin (assessed by dimethyl
derivative) [212], Pitavastatin [214], Rifampin [216]

OATP2B1
OATP-B

SLCO2B1
(SLC21A9)

BSP; DHEAS; estrone 3-sulfate [282], Fluvastatin [101]

OAT2 SLC22A7 5-Fluorouracil; allopurinol; L-ascorbic acid; bumetanide;

DHEAS; estrone 3-sulfate; glutarate [11], Erythromycin
[178], Methotrexate [10], Prostaglandin E 2 [11,17],
Prostaglandin F 2 [14], Ranitidine [287], Salicylate
(controversial) [12], Tetracycline [221], Theophylline
[178], Zidovudine [222]

OCT1 SLC22A1 Acyclovir, ganciclovir [222], Azidoprocainamide

methoiodide; n -methylquinidine; n - methylquinine;
tributylmethylammonium [223], Choline [224], Imatinib
[225], Metformin [226], MPP + ; N -methylnicotinamide;
tetraethylammonium [227,228,288], Famotidine,
ranitidine [179], Prostaglandin E 2 , prostaglandin F 2 [17]

OCT3
EMT

SLC22A3 Adrenaline, noradrenaline, tyramine [229], Agmatine,

MPP + ; tetraethylammonium [230-232], Atropine,
etilefrine [289], Histamine [224]

a BQ-123, [cyclo(D-Trp-D-Asp-L-Pro-D-Val-L-Leu)]; DPDPE, [D-penicillamine 2 , 5 ]-enkephalin; E 2 17G,
estradiol-17 ( -D-glucuronide); T 3 ,T 4 , thyroid hormones; LTC 4 , leukotriene C 4 ;MPP + , 1-methyl-4-
phenylpyridinium.