ArticleDrug metabolism and disposition: the biological fate of chemicals2012
Electrophysiological characterization of the polyspecific organic cation transporter plasma membrane monoamine transporter.
Article in Drug metabolism and disposition: the biological fate of chemicals, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 31 citations in OpenAlex.
- Evaluation of systemic and brain pharmacokinetic parameters for repurposing metformin using intravenous bolus administration.The Journal of pharmacology and experimental therapeutics · 2025Article
- Cortical and Striatal Astrocytes of Neonatal Rats Display Distinct Molecular and Pharmacological Characteristics of Dopamine Uptake.International journal of molecular sciences · 2024Article
- Dopamine internalization via UptakeFrontiers in pharmacology · 2024Article
- The Plasma Membrane Monoamine Transporter is Highly Expressed in Neuroblastoma and Functions as an mIBG Transporter.The Journal of pharmacology and experimental therapeutics · 2023Article
- Choroid Plexus and Drug Removal Mechanisms.The AAPS journal · 2021Review
- Brain Plasma Membrane Monoamine Transporter in Health and Disease.Handbook of experimental pharmacology · 2021Article
- General Overview of Organic Cation Transporters in Brain.Handbook of experimental pharmacology · 2021Article
- Region-specific blood-brain barrier transporter changes leads to increased sensitivity to amisulpride in Alzheimer's disease.Fluids and barriers of the CNS · 2019Article
- Bidirectional transport of 2-chloroadenosine by equilibrative nucleoside transporter 4 (hENT4): Evidence for allosteric kinetics at acidic pH.Scientific reports · 2019Article
- Constitutive plasma membrane monoamine transporter (PMAT, Slc29a4) deficiency subtly affects anxiety-like and coping behaviours.The European journal of neuroscience · 2018Article
- Renal Drug Transporters and Drug Interactions.Clinical pharmacokinetics · 2017Review
- Equilibrative nucleoside transporters-A review.Nucleosides, nucleotides & nucleic acids · 2017Review
- Organic cation transporter 1 (OCT1) is involved in pentamidine transport at the human and mouse blood-brain barrier (BBB).PloS one · 2017Article
- The plasma membrane monoamine transporter (PMAT): Structure, function, and role in organic cation disposition.Clinical pharmacology and therapeutics · 2016Review
- Polyspecific organic cation transporters and their impact on drug intracellular levels and pharmacodynamics.Pharmacological research · 2016Review
- Coexistence of passive and proton antiporter-mediated processes in nicotine transport at the mouse blood-brain barrier.The AAPS journal · 2013Article
- Impaired monoamine and organic cation uptake in choroid plexus in mice with targeted disruption of the plasma membrane monoamine transporter (Slc29a4) gene.The Journal of biological chemistry · 2013Article
- Residue Ile89 in human plasma membrane monoamine transporter influences its organic cation transport activity and sensitivity to inhibition by dilazep.Biochemical pharmacology · 2012Article
- Expression Profiling of Solute Carrier Gene Families at the Blood-CSF Barrier.Frontiers in pharmacology · 2012Article
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 2 countries.
Funding
Abstract
Plasma membrane monoamine transporter (PMAT) is a polyspecific organic cation (OC) transporter that transports a variety of endogenous biogenic amines and xenobiotic cations. Previous radiotracer uptake studies showed that PMAT-mediated OC transport is sensitive to changes in membrane potential and extracellular pH, but the precise role of membrane potential and protons on PMAT-mediated OC transport is unknown. Here, we characterized the electrophysiological properties of PMAT in Xenopus laevis oocytes using a two-microelectrode voltage-clamp approach. PMAT-mediated histamine uptake is associated with inward currents under voltage-clamp conditions, and the currents increased in magnitude as the holding membrane potential became more negative. A similar effect was also observed for another cation, nicotine. Substrate-induced currents were largely independent of Na+ but showed strong dependence on membrane potential and pH of the perfusate. Detailed kinetic analysis of histamine uptake revealed that the energizing effect of membrane potentials on PMAT transport is mainly due to an augmentation of Imax with little effect on K0.5. At most holding membrane potentials, Imax at pH 6.0 is approximately 3- to 4-fold higher than that at pH 7.5, whereas K0.5 is not dependent on pH. Together, these data unequivocally demonstrate PMAT as an electrogenic transporter and establish the physiological inside-negative membrane potential as a driving force for PMAT-mediated OC transport. The important role of membrane potential and pH in modulating the transport activity of PMAT toward OCs suggests that the in vivo activity of PMAT could be regulated by pathophysiological processes that alter physiological pH or membrane potential.
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