ArticleBritish journal of pharmacology2012
S(+)amphetamine induces a persistent leak in the human dopamine transporter: molecular stent hypothesis.
Article in British journal of pharmacology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Who cites it
23 citing papers in PubMed, 31 citations in OpenAlex.
- Electrophysiological Methods to Explore the Function of Monoamine Transporters.Advances in neurobiology · 2025Review
- Substrate Binding and Conformational Dynamics of the Monoamine Transporters.Advances in neurobiology · 2025Review
- Chronic Administration of Lisdexamfetamine Induces Apoptosis and Inflammation and Reduces Sperm Quality in Adult Male Rats.Reproductive sciences (Thousand Oaks, Calif.) · 2024Article
- Multi-modal antidepressant-like action of 6- and 7-chloro-2-aminodihydroquinazolines in the mouse tail suspension test.Psychopharmacology · 2019Article
- DARK Classics in Chemical Neuroscience: Cathinone-Derived Psychostimulants.ACS chemical neuroscience · 2018Review
- "Ecstasy" to addiction: Mechanisms and reinforcing effects of three synthetic cathinone analogs of MDMA.Neuropharmacology · 2018Article
- A kinetic account for amphetamine-induced monoamine release.The Journal of general physiology · 2018Article
- N-Alkylated Analogs of 4-Methylamphetamine (4-MA) Differentially Affect Monoamine Transporters and Abuse Liability.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2017Article
- Utility of preclinical drug versus food choice procedures to evaluate candidate medications for methamphetamine use disorder.Annals of the New York Academy of Sciences · 2017Review
- Electrophysiological Actions of Synthetic Cathinones on Monoamine Transporters.Current topics in behavioral neurosciences · 2017Article
- Dissociable effects of the prodrug phendimetrazine and its metabolite phenmetrazine at dopamine transporters.Scientific reports · 2016Article
- Chloride requirement for monoamine transporters.Pflugers Archiv : European journal of physiology · 2016Review
- A current view of serotonin transporters.F1000Research · 2016Review
- Amphetamine activates calcium channels through dopamine transporter-mediated depolarization.Cell calcium · 2015Article
- Comments on 'A quantitative model of amphetamine action on the serotonin transporter', by Sandtner et al., Br J Pharmacol 171: 1007-1018.British journal of pharmacology · 2015Article
- The conservative view: is it necessary to implant a stent into the dopamine transporter?British journal of pharmacology · 2015Article
- Structural analysis of dopamine- and amphetamine-induced depolarization currents in the human dopamine transporter.ACS chemical neuroscience · 2015Article
- Amphetamines, new psychoactive drugs and the monoamine transporter cycle.Trends in pharmacological sciences · 2015Review
- Intracellular methamphetamine prevents the dopamine-induced enhancement of neuronal firing.The Journal of biological chemistry · 2014Article
- Fishing for holes in transporters: how protons breach the Na/K pump security gates.The Journal of general physiology · 2014Article
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
Abstract
background and purposeWherever they are located, dopamine transporters (DATs) clear dopamine (DA) from the extracellular milieu to help regulate dopaminergic signalling. Exposure to amphetamine (AMPH) increases extracellular DA in the synaptic cleft, which has been ascribed to DAT reverse transport. Increased extracellular DA prolongs postsynaptic activity and reinforces abuse and hedonic behaviour. EXPERIMENTAL APPROACH: Xenopus laevis oocytes expressing human (h) DAT were voltage-clamped and exposed to DA, R(-)AMPH, or S(+)AMPH. KEY
resultsAt -60mV, near neuronal resting potentials, S(+)AMPH induced a depolarizing current through hDAT, which after removing the drug, persisted for more than 30 min. This persistent leak in the absence of S(+)AMPH was in contrast to the currents induced by R(-)AMPH and DA, which returned to baseline immediately after their removal. Our data suggest that S(+)AMPH and Na(+) carry the initial S(+)AMPH-induced current, whereas Na+ and Cl(-) carry the persistent leak current. We propose that the persistent current results from the internal action of S(+)AMPH on hDAT because the temporal effect was consistent with S(+)AMPH influx, and intracellular S(+)AMPH activated the effect. The persistent current was dependent on Na(+) and was blocked by cocaine. Intracellular injection of S(+)AMPH also activated a DA-induced persistent leak current. CONCLUSIONS AND IMPLICATIONS: We report a hitherto unknown action of S(+)AMPH on hDAT that potentially affects AMPH-induced DA release. We propose that internal S(+)AMPH acts as a molecular stent that holds the transporter open even after external S(+)AMPH is removed. Amphetamine-induced persistent leak currents are likely to influence dopaminergic signalling, DA release mechanisms, and amphetamine abuse.
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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.