ArticleThe AAPS journal2013
Coexistence of passive and proton antiporter-mediated processes in nicotine transport at the mouse blood-brain barrier.
Article in The AAPS journal, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 47 citations in OpenAlex.
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- Prediction of blood-brain barrier and Caco-2 permeability through the Enalos Cloud Platform: combining contrastive learning and atom-attention message passing neural networks.Journal of cheminformatics · 2025Article
- Brain endothelial permeability, transport, and flow assessed over 10 orders of magnitude using the in situ brain perfusion technique.Fluids and barriers of the CNS · 2024Article
- An extended substrate spectrum of the proton organic cation antiporter and relation to other cation transporters.Basic & clinical pharmacology & toxicology · 2024Article
- Natural Compounds as Inhibitors of Aβ Peptide and Tau Aggregation.CNS & neurological disorders drug targets · 2024Review
- A memory-improving dipeptide, Tyr-Pro, can reach the mouse brain after oral administration.Scientific reports · 2023Article
- Drug Permeability: From the Blood-Brain Barrier to the Peripheral Nerve Barriers.Advanced therapeutics · 2023Article
- Use of the head-twitch response to investigate the structure-activity relationships of 4-thio-substituted 2,5-dimethoxyphenylalkylamines.Psychopharmacology · 2023Article
- Proteomics-Based Transporter Identification by the PICK Method: Involvement of TM7SF3 and LHFPL6 in Proton-Coupled Organic Cation Antiport at the Blood-Brain Barrier.Pharmaceutics · 2022Article
- Pharmacophore-Based Discovery of Substrates of a Novel Drug/Proton-Antiporter in the Human Brain Endothelial hCMEC/D3 Cell Line.Pharmaceutics · 2022Article
- Substrate-DependentInternational journal of molecular sciences · 2021Article
- Rational Constructed Ultra-Small Iron Oxide Nanoprobes Manifesting High Performance forNanomaterials (Basel, Switzerland) · 2021Article
- Involvement of a Novel Organic Cation Transporter in Paeonol Transport Across the Blood-Brain Barrier.Biomolecules & therapeutics · 2019Article
- Imperatorin is Transported through Blood-Brain Barrier by Carrier-Mediated Transporters.Biomolecules & therapeutics · 2017Article
- Diphenhydramine as a selective probe to study HJournal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2017Article
- Blood-brain and retinal barriers show dissimilar ABC transporter impacts and concealed effect of P-glycoprotein on a novel verapamil influx carrier.British journal of pharmacology · 2016Article
- A polyspecific drug/proton antiporter mediates diphenhydramine and clonidine transport at the mouse blood-retinal barrier.British journal of pharmacology · 2015Article
- Pharmacophore-based discovery of inhibitors of a novel drug/proton antiporter in human brain endothelial hCMEC/D3 cell line.British journal of pharmacology · 2015Article
- Inside-out neuropharmacology of nicotinic drugs.Neuropharmacology · 2015Review
- Transporter-Mediated Disposition of Opioids: Implications for Clinical Drug Interactions.Pharmaceutical research · 2015Review
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Nicotine, the main tobacco alkaloid leading to smoking dependence, rapidly crosses the blood-brain barrier (BBB) to become concentrated in the brain. Recently, it has been shown that nicotine interacts with some organic cation transporters (OCT), but their influence at the BBB has not yet been assessed in vivo. In this study, we characterized the transport of nicotine at the mouse luminal BBB by in situ brain perfusion. Its influx was saturable and followed the Michaelis-Menten kinetics (K(m)=2.60 mM, V(max)=37.60 nmol/s/g at pH 7.40). At its usual micromolar concentrations in the plasma, most (79%) of the net transport of nicotine at the BBB was carrier-mediated, while passive diffusion accounted for 21%. Studies on knockout mice showed that the OCT Oct1-3, P-gp, and Bcrp did not alter [(3)H]-nicotine transport at the BBB. Neither did inhibiting the transporters Mate1, Octn, or Pmat. The in vivo manipulation of intracellular and/or extracellular pH, the chemical inhibition profile, and the trans-stimulation experiments demonstrated that the nicotine transporter at the BBB shared the properties of the clonidine/proton antiporter. The molecular features of this proton-coupled antiporter have not yet been identified, but it also transports diphenhydramine and tramadol and helps nicotine cross the BBB at a faster rate and to a greater extent. The pharmacological inhibition of this nicotine/proton antiporter could represent a new strategy to reduce nicotine uptake by the brain and thus help curb addiction to smoking.
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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.