ArticlePharmaceutical research2022
High Throughput Screening of a Prescription Drug Library for Inhibitors of Organic Cation Transporter 3, OCT3.
Article in Pharmaceutical research, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 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
14 citing papers in PubMed, 21 citations in OpenAlex.
- The 2-Amino-3,4-dihydroquinazoline Molecular Scaffold as Novel OCT3 Inhibitor.ACS chemical neuroscience · 2026Article
- Proteomic profiling reveals age-related changes in transporter proteins in the human blood-brain barrier.Scientific reports · 2025Article
- Cardiac Uptake of the Adrenergic Imaging AgentDrug metabolism and disposition: the biological fate of chemicals · 2024Article
- Organic cation transporters in psychiatric and substance use disorders.Pharmacology & therapeutics · 2024Review
- Cardiac contraction and relaxation are regulated by distinct subcellular cAMP pools.Nature chemical biology · 2024Article
- Stereoselectivity in Cell Uptake by SLC22 Organic Cation Transporters 1, 2, and 3.Journal of medicinal chemistry · 2023Article
- Stereoselective Inhibition of High- and Low-Affinity Organic Cation Transporters.Molecular pharmaceutics · 2023Article
- TICBase: Integrated Resource for Data on Drug and Environmental Chemical Interactions with Mammalian Drug Transporters.Clinical pharmacology and therapeutics · 2023Article
- Illuminating the monoamine transporters: Fluorescently labelled ligands to study dopamine, serotonin and norepinephrine transporters.Basic & clinical pharmacology & toxicology · 2023Review
- The Influence ofDiabetes, metabolic syndrome and obesity : targets and therapy · 2023Article
- Article
- Stereoselectivity in the Membrane Transport of Phenylethylamine Derivatives by Human Monoamine Transporters and Organic Cation Transporters 1, 2, and 3.Biomolecules · 2022Article
- A Historical Review of Brain Drug Delivery.Pharmaceutics · 2022Review
- Increased amisulpride serum concentration in a patient treated with concomitant pregabalin and trazodone: a case report.Therapeutic advances in psychopharmacology · 2022Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
8 authors at 3 institutions in 2 countries.
Funding
Abstract
introductionThe organic cation transporter 3 (OCT3, SLC22A3) is ubiquitously expressed and interacts with a wide array of compounds including endogenous molecules, environmental toxins and prescription drugs. Understudied as a determinant of pharmacokinetics and pharmacodynamics, OCT3 has the potential to be a major determinant of drug absorption and disposition and to be a target for drug-drug interactions (DDIs). GOAL: The goal of the current study was to identify prescription drug inhibitors of OCT3.
methodsWe screened a compound library consisting of 2556 prescription drugs, bioactive molecules, and natural products using a high throughput assay in HEK-293 cells stably expressing OCT3.
resultsWe identified 210 compounds that at 20 μM inhibit 50% or more of OCT3-mediated uptake of 4-Di-1-ASP (2 μM). Of these, nine were predicted to inhibit the transporter at clinically relevant unbound plasma concentrations. A Structure-Activity Relationship (SAR) model included molecular descriptors that could discriminate between inhibitors and non-inhibitors of OCT3 and was used to identify additional OCT3 inhibitors. Proteomics of human brain microvessels (BMVs) indicated that OCT3 is the highest expressed OCT in the human blood-brain barrier (BBB).
conclusionsThis study represents the largest screen to identify prescription drug inhibitors of OCT3. Several are sufficiently potent to inhibit the transporter at therapeutic unbound plasma levels, potentially leading to DDIs or off-target pharmacologic effects.
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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 Socratic graph.