hOATP1A2 (SLCO1A2)
➦ The organic anion transporting polypeptide OATP1A2 (formerly termed OATP or OATP-A) was the first member of the human OATP family to be cloned and functionally characterized. OATP1A2 protein is found on the luminal membrane of the brain capillary endothelial cells, which make up the blood-brain barrier, apical membranes of cholangiocytes in the liver, and apical membrane of the distal nephrons in the kidney.
| Main localization: | Brain, kidney, liver |
| Transporter assay: | Uptake transporter assay |
| Probe substrates: | Estrone-3-sulfate, trospium |
| Probe inhibitors: | Rifampicin, verapamil |
| Regulatory relevance: | − |
| Important interacting drugs: | Trospium, fexofenadine, pitavastatin, rosuvastatin, quabain, BSP, cyclosporine, naringin, rifampicin, ritonavir, saquinavir, verapamil |
➦ Inhibitory effect on OATP1A2-mediated trospium uptake by various inhibitors (100 µM)
