hOCT3 (SLC22A3)

The human organic cation transporter 3 (OCT3) has a broad tissue distribution and was detected e.g. in brain, kidney, heart, liver and placenta as well as in several cancer cell, especially in renal carcinoma cells. OCT3 (SLC22A3), also designated as extraneuronal monoamine transporter (EMT) participates in the cellular uptake and elimination of various cationic substrates like catecholamines and histamine as well as in handling of therapeutically important agents e.g. cytostatics. Impaired expression or function of OCT3 seems to have significant impact on the pharmacokinetics of metformin.

Main localization:
Liver, placenta, brain, kidney, heart
Transporter assay:
Uptake transporter assay
Probe substrates:
1-methyl-4-phenyl-pyridinium (MPP), metformin
Probe inhibitors:
Decynium22, quinine
Regulatory relevance:
Important interacting drugs:
Metformin, quinine, quinidine, etilefrin, lidocaine, memantine, ranitidine, pentamidine, oxaliplatin, famotidine, furamidine, prazosin, phenoxybenzamine
From other species:

Concentration dependent inhibition of hOCT3-mediated MPP uptake by the probe inhibitor decynium22

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