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)
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