ArticleMolecular psychiatry2021
Amphetamines signal through intracellular TAAR1 receptors coupled to Gα
Article in Molecular psychiatry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 55 papers.
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Who cites it
55 citing papers in PubMed, 87 citations in OpenAlex.
- Trace amine-associated receptor gene polymorphism increases drug craving in individuals with methamphetamine dependence.PloS one · 2019Trial
- A comprehensive overview of the biological foundations of ADHD.Bioscience reports · 2026Review
- Localization, trafficking, and signaling of trace amine-associated receptor 2 in mouse neuroblastoma cells.Cellular signalling · 2026Article
- Potential of Small Molecule TAAR-1 Agonists for the Therapy of Neurodegenerative Psychosis: A Medicinal Chemistry Perspective.Mini reviews in medicinal chemistry · 2026Review
- The Role of Trace Amine-Associated Receptor 1 (TAAR1) in the Pathophysiology and Treatment of Depression.Current neuropharmacology · 2026Review
- Multidimensional Evaluation of Lisdexamfetamine: Pharmacology, Therapeutic Use, Toxicity and Forensic Implications.Basic & clinical pharmacology & toxicology · 2025Review
- Revisiting the Role of Serotonin in Attention-Deficit Hyperactivity Disorder: New Insights from Preclinical and Clinical Studies.Clinical drug investigation · 2025Review
- Trace amine-associated receptor 1 agonists differentially regulate dopamine transporter function.Molecular pharmacology · 2025Article
- Dynamic Regulation of Cholesterol Metabolism Genes in Dopaminergic Neurons following Methamphetamine Treatment as Revealed by Single-Nucleus RNA Sequencing.bioRxiv : the preprint server for biology · 2025Article
- Absence of TAAR1 function increases methamphetamine-induced excitability of dorsal raphe serotonin neurons and drives binge-level methamphetamine intake.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2025Article
- Trace amine-associated receptor 1 (TAAR1): an emerging therapeutic target for neurodegenerative, neurodevelopmental, and neurotraumatic disorders.Naunyn-Schmiedeberg's archives of pharmacology · 2025Review
- Reappraisal of the mechanism of cardiovascular responses to sympathomimetic amines in anaesthetised rats: dual αNaunyn-Schmiedeberg's archives of pharmacology · 2025Article
- Regulation of Dopamine Transporter Surface Expression.Advances in neurobiology · 2025Review
- Trace Amine-associated Receptor 1: Role in the Implementation of Neuroprotective Signaling Pathways.International journal of molecular and cellular medicine · 2025Review
- Monoamine transporter ubiquitination and inward-open conformation synergistically maximize transporter endocytosis.Science advances · 2024Article
- Article
- Enantiomeric contributions to methamphetamine's bidirectional effects on basal and fentanyl-depressed respiration in mice.Pharmacology, biochemistry, and behavior · 2024Article
- Molecular basis of human trace amine-associated receptor 1 activation.Nature communications · 2024Article
- TAAR1 as an emerging target for the treatment of psychiatric disorders.Pharmacology & therapeutics · 2024Review
- Article
Corrections and comments
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Authors and funding
7 authors at 3 institutions in 2 countries.
Funding
Abstract
The extensive use of amphetamines to treat attention deficit hyperactivity disorders in children provides a compelling rationale for understanding the mechanisms of action of amphetamines and amphetamine-related drugs. We have previously shown that acute amphetamine (AMPH) regulates the trafficking of both dopamine and glutamate transporters in dopamine neurons by increasing activation of the small GTPase RhoA and of protein kinase A. Here we demonstrate that these downstream signaling events depend upon the direct activation of a trace amine-associated receptor, TAAR1, an intracellular G-protein coupled receptor (GPCR) that can be activated by amphetamines, trace amines, and biogenic amine metabolites. Using cell lines and mouse lines in which TAAR1 expression has been disrupted, we demonstrate that TAAR1 mediates the effects of AMPH on both RhoA and cAMP signaling. Inhibition of different Gα signaling pathways in cell lines and in vivo using small cell-permeable peptides confirms that the endogenous intracellular TAAR1 couples to G
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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 OpenQuestion graph.