ArticleDrug metabolism and disposition: the biological fate of chemicals2014
Common drugs inhibit human organic cation transporter 1 (OCT1)-mediated neurotransmitter uptake.
Article in Drug metabolism and disposition: the biological fate of chemicals, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 36 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
36 citing papers in PubMed, 65 citations in OpenAlex.
- Trial
- A drug-drug interaction study to evaluate the impact of peficitinib on OCT1- and MATE1-mediated transport of metformin in healthy volunteers.European journal of clinical pharmacology · 2020Trial
- Putative new biomarkers for renal transporter-mediated drug-drug interactions: Characterization as substrates of organic cation transporter 2, multidrug and toxin extrusion protein 1, and other important drug transporters.Drug metabolism and disposition: the biological fate of chemicals · 2025Article
- Clozapine impaired glucose-stimulated insulin secretion partly by increasing plasma 5-HT levels due to the inhibition of OCT1-mediated hepatic 5-HT uptake in mice.Acta pharmacologica Sinica · 2025Article
- OCT1 (SLC22A1) transporter kinetics and regulation in primary human hepatocyte 3D spheroids.Scientific reports · 2024Article
- Article
- Organic cation transporters in psychiatric and substance use disorders.Pharmacology & therapeutics · 2024Review
- A chemical probe unravels the reactive proteome of health-associated catechols.Chemical science · 2023Article
- Molecular basis of polyspecific drug and xenobiotic recognition by OCT1 and OCT2.Nature structural & molecular biology · 2023Article
- Molecular basis of polyspecific drug binding and transport by OCT1 and OCT2.bioRxiv : the preprint server for biology · 2023Article
- Human Hepatic Transporter Signature Peptides for Quantitative Targeted Absolute Proteomics: Selection, Digestion Efficiency, and Peptide Stability.Pharmaceutical research · 2022Article
- Antioxidant and Neuroprotective Effects of Paeonol against Oxidative Stress and Altered Carrier-Mediated Transport System on NSC-34 Cell Lines.Antioxidants (Basel, Switzerland) · 2022Article
- Dengue Virus Replication Is Associated with Catecholamine Biosynthesis and Metabolism in Hepatocytes.Viruses · 2022Article
- Association of Hepatitis C Virus Replication with the Catecholamine Biosynthetic Pathway.Viruses · 2021Article
- Differential Serotonin Uptake Mechanisms at the Human Maternal-Fetal Interface.International journal of molecular sciences · 2021Article
- Transport of Drugs and Endogenous Compounds Mediated by Human OCT1: Studies in Single- and Double-Transfected Cell Models.Frontiers in pharmacology · 2021Review
- Organic Cation Transporter Expression and Function in the CNS.Handbook of experimental pharmacology · 2021Article
- General Overview of Organic Cation Transporters in Brain.Handbook of experimental pharmacology · 2021Article
- Organic Cation Transporters in the Lung-Current and Emerging (Patho)Physiological and Pharmacological Concepts.International journal of molecular sciences · 2020Review
- OATP1B3 Expression and Function is Modulated by Coexpression with OCT1, OATP1B1, and NTCP.Drug metabolism and disposition: the biological fate of chemicals · 2020Article
Corrections and comments
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Authors and funding
3 authors at 2 institutions in 1 country.
Funding
Abstract
The human organic cation transporter 1 (OCT1) is a polyspecific transporter involved in the uptake of positively charged and neutral small molecules in the liver. To date, few endogenous compounds have been identified as OCT1 substrates; more importantly, the effect of drugs on endogenous substrate transport has not been examined. In this study, we established monoamine neurotransmitters as substrates for OCT1, specifically characterizing serotonin transport in human embryonic kidney 293 cells. Kinetic analysis yielded a Km of 197 micomolar and a Vmax of 561 pmol/mg protein/minute for serotonin. Furthermore, we demonstrated that serotonin uptake was inhibited by diphenhydramine, fluoxetine, imatinib, and verapamil, with IC50 values in the low micromolar range. These results were recapitulated in primary human hepatocytes, suggesting that OCT1 plays a significant role in hepatic elimination of serotonin and that xenobiotics may alter the elimination of endogenous compounds as a result of interactions at the transporter level.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.