Table II.
Characteristics of the organic anion transporter (OAT) family.
| Gene | Protein | mRNA expression |
Tissue distribution |
Localization | Km (μM) | Substrates/inhibitors |
|---|---|---|---|---|---|---|
| SLC22A6 | rOat1 | Kidney, brain, CPa |
Kidney (cortex> medulla), brain |
Basolateral PT | PAH (11–85.1), ACV (242), adefovir (270), cidofovir (238), AZT (68), OTA (0.57, 2.1), DNP-NAC (2), PMEA (30) |
2,4-D, antiviral agents, PGE2, PGF2α, α-KG, urate, NSAIDs, MTX, β-lactam antibiotics, ACE inhibitors, uraemic toxins, cAMP, cGMP, folate, acetazol- amide, acetylsalicylate, benzylpenecillin (penicillin G), cephaloridine, furosemide, indomethacin, lamivudine, PMEDAP, PMEG, salicylate, stavudine, trifluridine, zalcitabine |
| mOat1 | Kidney, brain, CPa |
Kidney, brain | Basolateral PT | PAH (37, 162) | Ascorbate, captopril, carprofen, cisplatin, diclofenac, enalapril, folate, indomethacin |
|
| hOAT1 | Kidney, brain, CPa |
Kidney, brain, placenta |
Basolateral PT | PAH (3.9–22), ACV (342.3), adefovir (23.8, 30), cidofovir (46, 58), Ganciclovir (896), AZT (45.9), 6- CF (3.93), GA (10.7), MTX (553.8), OTA (0.42), PGE2 (0.97), PGF2α (0.58) |
2,4-D, antiviral agents, α-KG, NSAIDs, uraemic toxins, fluorescein, indole acetate, indoxyl sulfate, penicillin G, BSP, cimetidine, diclofenac, DMPS, furosemide, phenol red, PMEDAP, PMEG, probenecid, tetracycline, doxycycline, bumetanide, betamipron, cefoperazone |
|
| fOat1 | Kidney | Kidney | PAH (21–58) | ES, 2,4-D, antiviral agents (adefovir, cidoforvir), OTA, bumetanide, cimetidine, didanosine, DMPS, ethacrynate, OTA, PMEDAP, PMEG, tienilate |
||
| ceOat1 | PAH (430) | Ascorbate, penicillin G, folate, furosemide |
||||
| rbOat1 | Kidney | Kidney | PAH (15.6) | DMPS, probenecid | ||
| pOat1 | Kidney | PAH (3.7) | Glutarate, probenecid | |||
| mkOat1 | Kidney | PAH (10), 2,4-D (3), hippurate (12.2), indoleacetate (23.6), indoxyl sulfate (32.9), CMPF (85.3) |
Probenecid, furosemide, bumetanide, chlorothiazide, α-KG, penicillin G |
|||
| SLC22A7 | rOat2 | Liver (M:L>K)b, kidney (F:K>L)b, CPa |
Liver, kidney, adipose tissue |
Sinusoidal, apical late PT, TAL and CD |
PGE2 (38.5), salicylate (81/88.9), α-KG (17.8), AZT (26), 2, 3-di- deoxycytidine (3, 080), indomethacin (0.37) |
Glutarate, methotrexate, bumetanide, PAH, PGE2, cAMP, DHEAS, tetracycline, NSAIDs, AZT, MTX, zalcitabine, acetylsalicylate |
| mOat2 | Kidney (F>M), liver, CPa |
Kidney, liver | Apical late PT | PGE2 (0.005), GA (15.8), bumetanide (9) |
PGE2, tetracycline, allopurinol, PAH, α-KG, MTX, OTA, valproate |
|
| hOAT2 | Liver, kidney | Liver, kidney | Sinusoidal, basolateral PT | PGE2 (0.72), PGF2α (0.43), salicylate (3.9), GA (0.43), AZT (26.8), tetracycline (439.9) |
Glutarate, α-KG, MTX, PAH, cAMP | |
| rbOat2 | Kidney, liver, CPa |
|||||
| SLC22A8 | rOat3 | Kidney, liver, CPa |
Liver, kidney, brain |
Basolateral PT | PAH (60–278), ES (2.3-5.3), benzylpenicillin (82.6), 2,4-D (20), cimetidine (40), E2-17-β-G (8.43), indoxyl sulfate (158), OTA (0.74), pravastatin (13.4) |
cAMP, cGMP, glutarate, oestradiol glucuoronide, MTX, MPP |
| mOat3 | Kidney, brain, CPa |
Kidney, brain, eye |
Apical CP | 6-Mercaptopurine (4), 5-fluorouracil (0.054), L-carnitine (0.062) |
ES, PAH, PGE2, PGF2α, allopurinol | |
| hOAT3 | Kidney, brain, skeletal muscle, adrenal tissue |
Kidney, brain, skeletal muscle |
Basolateral PT | PAH (87.2), ES (3.1-9.5), cortisol (2.4), PGE2 (0.35), PGF2a (1.1), AZT (145.1), cimetidine (57.4), MTX (10.9), OTA (0.75), tetracycline (566.2) |
2,4-D, cortisol, cAMP, DHEAS, oestradiol glucuronide, urate, salicylate, GA, salicylate, taurocholate, valacyclovir |
|
| rbOat3 | Kidney | Kidney | ES (4.5) | |||
| pOat3 | Kidney | ES (7.8) | Glutarate, DHEAS | |||
| SLC22A8 | mkOat3 | ES (10.6), penicillin G (49.2), cimetidine (68.5), CMPF (18.6) |
PAH, probenecid, furosemide, bumetanide, chlorothiazide, α-KG, penicillin G |
|||
| SLC22A11 | hOAT4 | Kidney, placenta, adrenal tissues |
Kidney | Apical PT, basal membrane of syncytiotrophoblast |
ES (1, 4.2), 6-CF (108.3), DHEAS (0.6), OTA (23), PGE2 (0.15), PGF2a (692), zonampenal (215), MTX (18) |
tetracycline, steroid sulfates (β-oestradiol-3, 17-disulfate, 17-β-oestradiol 3-disulfate, β-oestradiol 3-disulfate, AZT, cimetidine, urate |
| SLC22A12 | rUrat1 | Kidney, liver, CPa |
||||
| mUrat1 | Kidney | Kidney | Apical PT | Urate (1, 213) | Lactate, nicotinate | |
| hUrat1 | Kidney | Kidney | Apical PT | Urate (199, 371) | PZA, nicotinate | |
| rbUrat1 | Kidney, liver, CPa |
|||||
| SLC22A19 | rOat5 | Kidney | Kidney | Apical PT, outer- and juxta-medullary cortex |
OTA (0.34), ES (18.9), DHEAS (2.3) |
Sulfate conjugates |
| mOat5 | Kidney | Kidney | S2–S3 PT, glomeruli, CCD, MAL |
OTA (2), ES (2.2), DHEAS (3.8) | Sulfate conjugates | |
| rbOat5 | Kidney, liver, CPa |
|||||
| SLC22A20 | mOat6 | Olfactory mucosa |
Olfactory mucosa, vomeronasal organ |
ES (45–110) | Probenecid, 2,4-D, penicillin G, salicylate, propionate, 2 and 3-methylbutyrates, benzoate |
|
| SLC22A9 | hOAT7 | Liver | Liver | Sinusoidal | ES (8.7), DHEAS (2.2) | β-oestradiol sulfate, BSP, SCFAs |
Note:
a
CP, choroid plexus.
b
M, male; F, female; L, liver; K, kidney.