Table 5.
OATP Substrates
|
Table 2 substrates transported by the deferent human OATPs
| |||
|---|---|---|---|
| OATP1A2 | OATP1B1 | OATP1B3 | OATP1CJ |
| Hormones and conjugates | Hormones and conjugates | Hormones and conjugates | Hormones and conjugates |
| Estradiol-17 P-glucuronide | Estradiol-17 (3-glucuronide) | Estradiol-17 (3-glucuronide) | Estradiol-17 (3-glucuronide) |
| Estrone-3-sulfate | Estrone-3-sulfate | Estrone-3-sulfate | Estrone-3-sulfate |
| DHEA-S | Thyroxine (T4) | DHEA-S | Thyroxine (T4) |
| Reverse triiodothyronine (TT) | Triiodothyronine (T3) | Testosterone | Triiodothyronine (T3) |
| Thyroxine (T4) | DHEA-S | Drags | Reverse triiodothyronine (rT3) |
| Triiodothyronine (T3) | Prostaglandins | Atrasentan, Bosentan | Thyroxine sulfate (T4S) |
| Prostaglandins | Prostaglandin Ei | Cefadroxil, Cefazolin | Others |
| Prostaglandin £2 | Bile acids | Cephalexin, Digoxin | BSP |
| Bile acids | Cholate | Enalapril, Fexofenadine | |
| Cholate | Taurocholate | Fluvastatin, Gimatecan | |
| Taurocholate | TUDCA | Lopinavir, Methotrexate | |
| Glycocholate | Drugs | Demethylphalloin | |
| TCDCA | Atorvastatin, Olmesartan | Paclitaxel, Docetaxel | |
| TUDCA | Bosentan, Phalloidin | Methotrexate, Imatinib | |
| Others | Caspofungin, Pitavastatin | Olmesartan, Phalloidin | |
| DPDPE | Cefazolin, Pravastatin | Pitavastatin, Telmisartan | |
| Drugs | Cerivastatin, Rapamycin | Rapamycin, Rifampicin | |
| Acebutolol, Rosuvastatin | Darunavir, Rifampicin | Rosuvastatin, Valsartan | |
| Atenolol, Pitavastatin | Enalapril, Rosuvastatin | SN-38 | |
| Sotalol, Ouabain, Labetalol | Ezetimibe, Saquinavir | ||
| Deltorphin n, Nadolol | Flavopiridol, SN-38 | ||
| Ciprofloxacin, Talinolol | Fluvastatin, Temocapril | ||
| Fexofenadine, Saquinavir | Gimatecan, Troglitazone | ||
| Gatifloxacin, Darunavir | Lopinavir, Valsartan | ||
| Levofloxacin | Methotrexate | ||
| Imatinib, Methotrexate | |||
| OATP2A1 | OATP2B1 | OATP3A1 | OATP4A1 |
| Prostaglandins | Hormones and conjugates | Hormones and conjugates | Hormones and conjugates |
| Prostaglandin Ei | Estrone-3-sulfate | Thyroxine (T4) | Estradiol-17 (3-glucuronide) |
| Prostaglandin E2 | DHEA-S | Estrone-3 -sulfate | Estrone-3-sulfate |
| Prostaglandin Fj,, | Thyroxine (T4) | Prostaglandins | Thyroxine (T4) |
| Prostaglandin Hi | Prostaglandins | Prostaglandin Ei | Triiodothyronine (T3) |
| Prostaglandin D2 | Prostaglandin E2 | Prostaglandin E> | Reverse triiodothyronine (rT3 |
| 8-Iso-prostaglandin F2 << | Drags | Prostaglandin F2a | Bile acids |
| Others | Atorvastatin | Drugs | Taurocholate |
| Thromboxane B2 | Bosentan | Deltorphin BQ-123 | Prostaglandins |
| Drugs | Ezetimibe | Benzyl penicillin | Prostaglandin E > |
| Latanoprost | Fluvastatin | Others | Drugs |
| Glibenclamide | Vasopressin | Benzylpenicillin | |
| Pitavastatin | Arachidonic acid | Unoprostone metabolite | |
| Pitavastatin | |||
| Montelukast | |||
| Rosuvastatin | |||
| Talinolol | |||
Abbreviations: BSP, bromosulfophthalein; DHEA-S, dehydroepiandrosterone sulfate; DPDPE, [D-penicillamine 2,5] enkephalin Reprinted, with permission, from Ref. (418).