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To clarify inter-individual variation in the expression of organic cation transporter 1 (OCT1), the levels of OCT1 mRNA and protein from 65 human liver samples were examined by real-time PCR and Western blot analysis and were associated with OCT1 genotypes.
Sang-Seop Lee +2 more
exaly +3 more sources
Debrisoquine is a probe drug for in vivo phenotyping of human CYP2D6 metabolic activity. However, debrisoquine is positively charged under physiological conditions and it is unclear how it enters the hepatocytes to undergo CYP2D6 metabolism.
Jürgen Brockmöller, Mladen V Tzvetkov
exaly +2 more sources
Common genetic variants of the liver-specific human organic cation transporter 1 (OCT1; SLC22A1) have reduced transport capacity for substrates such as the antidiabetic drug metformin.
Per Artursson
exaly +2 more sources
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Gene, 2013
"OCT1" is used in the literature to describe two distinct genes and their resulting proteins, namely organic cation transporter 1 (encoded by SLC22A1) and octamer binding transcription factor 1 (encoded by POU2F1). The interchangeable use of "OCT1" is misleading and could result in erroneous research data.
Sandhya, Sreenivasan +1 more
openaire +2 more sources
"OCT1" is used in the literature to describe two distinct genes and their resulting proteins, namely organic cation transporter 1 (encoded by SLC22A1) and octamer binding transcription factor 1 (encoded by POU2F1). The interchangeable use of "OCT1" is misleading and could result in erroneous research data.
Sandhya, Sreenivasan +1 more
openaire +2 more sources
Can “specific” OCT1 inhibitors be used to determine OCT1 transporter activity toward imatinib?
Blood, 2013To the editor: The human organic cation transporter (OCT1) has been implicated in the uptake of imatinib into chronic myeloid leukemia (CML) cells.[1][1][⇓][2][⇓][3]-[4][4] Moreover, OCT1 expression or activity is thought to be a critical determinant of imatinib response and is considered ...
Burger, H (Hens) +3 more
openaire +2 more sources
Naunyn-Schmiedeberg's Archives of Pharmacology, 2021
Abstracts of the 87th Annual Meeting of the German Society for Experimental and Clinical Pharmacology and Toxicology (DGPT) with contribution of the Arbeitsgemeinschaft für Angewandte Humanpharmakologie e. V. (AGAH)
Meyer, M. J. +9 more
openaire +1 more source
Abstracts of the 87th Annual Meeting of the German Society for Experimental and Clinical Pharmacology and Toxicology (DGPT) with contribution of the Arbeitsgemeinschaft für Angewandte Humanpharmakologie e. V. (AGAH)
Meyer, M. J. +9 more
openaire +1 more source
Catecholamine transport by the organic cation transporter type 1 (OCT1) [PDF]
Liver and kidney extract adrenaline and noradrenaline from the circulation by a mechanism which does not seem to be one of the classical catecholamine transporters. The hypothesis that OCT1 is involved–the organic cation transporter type 1 which exists in rat kidney and liver–was tested.
Dirk Gründemann, E Schömig
exaly +3 more sources
Lamotrigine is a substrate for OCT1 in brain endothelial cells
Biochemical Pharmacology, 2012The mechanisms that underpin the passage of lamotrigine at the blood-brain barrier to its site of action in the brain is poorly understood. Lamotrigine has been postulated to be delivered to its site of action in the brain favourably despite its physicochemical properties.
Dickens, David +8 more
openaire +3 more sources
Xenobiotica, 2007
The contribution of organic cation transporters to the saturable component in the hepatic uptake of 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), cimetidine, and metformin was examined by the use of human/rat organic cation transporter (hOCT1/rOct1)-expressing cells and human/rat hepatocytes.
K-I, Umehara +3 more
openaire +2 more sources
The contribution of organic cation transporters to the saturable component in the hepatic uptake of 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), cimetidine, and metformin was examined by the use of human/rat organic cation transporter (hOCT1/rOct1)-expressing cells and human/rat hepatocytes.
K-I, Umehara +3 more
openaire +2 more sources
Relevance of the OCT1 transporter to the antineoplastic effect of biguanides
Biochemical and Biophysical Research Communications, 2011Epidemiologic and laboratory data suggesting that metformin has antineoplastic activity have led to ongoing clinical trials. However, pharmacokinetic issues that may influence metformin activity have not been studied in detail. The organic cation transporter 1 (OCT1) is known to play an important role in cellular uptake of metformin in the liver.
Eric D, Segal +5 more
openaire +2 more sources

