Catecholamine transport by the organic cation transporter type 1 (OCT1)

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Functional Properties of Organic Cation Transporter OCT1, Binding of Substrates and Inhibitors, and Presumed Transport Mechanism

Organic cation transporters (OCTs) of the SLC22 family mediate absorption, distribution and excretion of cationic drugs. The OCTs belong to the major facilitator superfamily (MFS) containing transporters with 12 pseudosymmetrically arranged transmembrane α-helices. Whereas most transporters of the MFS are substrate selective and secondary active, most transporters of the SLC22 family are polysp...

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Effect of genetic variation in the organic cation transporter 1 (OCT1) on metformin action.

Metformin is among the most widely prescribed drugs for the treatment of type 2 diabetes. Organic cation transporter 1 (OCT1) plays a role in the hepatic uptake of metformin, but its role in the therapeutic effects of the drug, which involve activation of AMP-activated protein kinase (AMPK), is unknown. Recent studies have shown that human OCT1 is highly polymorphic. We investigated whether OCT...

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Organic cation transporter 1 (OCT1) is involved in pentamidine transport at the human and mouse blood-brain barrier (BBB)

Pentamidine is an effective trypanocidal drug used against stage 1 Human African Trypanosomiasis (HAT). At the blood-brain barrier (BBB), it accumulates inside the endothelial cells but has limited entry into the brain. This study examined transporters involved in pentamidine transport at the human and mouse BBB using hCMEC/D3 and bEnd.3 cell lines, respectively. Results revealed that both cell...

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Regulation of basal core promoter activity of human organic cation transporter 1 (OCT1/SLC22A1).

Human organic cation transporter 1 (OCT1/SLC22A1) plays important roles in the hepatic uptake of cationic drugs. The functional characteristics of this transporter have been well evaluated, but molecular information regarding transcriptional regulation is limited. In the present study, therefore, we examined the gene regulation of OCT1 gene focusing on basal core expression. An approximately 2....

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Cellular uptake of imatinib into leukemic cells is independent of human organic cation transporter 1 (OCT1).

PURPOSE In addition to mutated BCR-ABL1 kinase, the organic cation transporter 1 (OCT1, encoded by SLC22A1) has been considered to contribute to imatinib resistance in patients with chronic myeloid leukemia (CML). As data are conflicting as to whether OCT1 transports imatinib and may serve as a clinical biomarker, we used a combination of different approaches including animal experiments to elu...

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ژورنال

عنوان ژورنال: British Journal of Pharmacology

سال: 1998

ISSN: 0007-1188

DOI: 10.1038/sj.bjp.0702065