ArticleInternational journal of molecular sciences2022
Substrates of the Human Brain Proton-Organic Cation Antiporter and Comparison with Organic Cation Transporter 1 Activities.
Article in International journal of molecular sciences, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed, 26 citations in OpenAlex.
- Sex-Dependent Effects of CYP2D6 on the Pharmacokinetics of Berberine in Humans.Clinical pharmacology and therapeutics · 2025Trial
- Intracerebral Distribution of Drugs with Diverse Blood-brain Barrier Transport Characteristics: In vivo Analysis using Brain Microdialysis in Cynomolgus Monkeys.Pharmaceutical research · 2026Article
- Acute hypobaric hypoxia attenuates the anti-fatigue effects of pitolisant by downregulating the expression of organic cation transporter 1 and P-glycoprotein.Frontiers in pharmacology · 2025Article
- Editorial: New approaches to overcome the blood-brain barrier for the treatment of CNS disorders.Frontiers in cellular neuroscience · 2025Article
- An extended substrate spectrum of the proton organic cation antiporter and relation to other cation transporters.Basic & clinical pharmacology & toxicology · 2024Article
- The putative proton-coupled organic cation antiporter is involved in uptake of triptans into human brain capillary endothelial cells.Fluids and barriers of the CNS · 2024Article
- Region-independent active CNS net uptake of marketed HFrontiers in cellular neuroscience · 2024Article
- Atypical Substrates of the Organic Cation Transporter 1.Biomolecules · 2022Article
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
Many organic cations (OCs) may be transported through membranes by a genetically still uncharacterized proton-organic cation (H + OC) antiporter. Here, we characterized an extended substrate spectrum of this antiporter. We studied the uptake of 72 drugs in hCMEC/D3 cells as a model of the human blood-brain barrier. All 72 drugs were tested with exchange transport assays and the transport of 26 of the drugs was studied in more detail concerning concentration-dependent uptake and susceptibility to specific inhibitors. According to exchange transport assays, 37 (51%) drugs were good substrates of the H + OC antiporter. From 26 drugs characterized in more detail, 23 were consistently identified as substrates of the H + OC antiporter in six different assays and transport kinetic constants could be identified with intrinsic clearances between 0.2 (ephedrine) and 201 (imipramine) mL × minute
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