Modulation of Monoamine Transporters by Common Biogenic Amines via Trace Amine-Associated Receptor 1 and Monoamine Autoreceptors in Human Embryonic Kidney 293 Cells and Brain Synaptosomes
@article{Xie2008ModulationOM, title={Modulation of Monoamine Transporters by Common Biogenic Amines via Trace Amine-Associated Receptor 1 and Monoamine Autoreceptors in Human Embryonic Kidney 293 Cells and Brain Synaptosomes}, author={Zhihua Xie and Susan Westmoreland and Gregory M. Miller}, journal={Journal of Pharmacology and Experimental Therapeutics}, year={2008}, volume={325}, pages={629 - 640} }
In brain monoaminergic systems, common biogenic amines, including dopamine, norepinephrine, and serotonin, serve as neurotransmitters. Monoamine autoreceptors provide feedback regulation in neurotransmitter release, and monoamine transporters clear the released neurotransmitters to control synaptic signaling. Recently, trace amine-associated receptor 1 (TAAR1) has been found to be expressed in brain monoaminergic nuclei and activated by common biogenic amines in vitro. This study used…
69 Citations
β-Phenylethylamine Alters Monoamine Transporter Function via Trace Amine-Associated Receptor 1: Implication for Modulatory Roles of Trace Amines in Brain
- Biology, ChemistryJournal of Pharmacology and Experimental Therapeutics
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Results reveal that β-PEA alters monoamine transporter function via interacting with TAAR1 but not monoamine autoreceptors, which may reveal a common mechanism by which trace amines exert modulatory effects on monoamine transporters in brain.
Trace amine-associated receptor 1 as a monoaminergic modulator in brain.
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Brain-Specific Overexpression of Trace Amine-Associated Receptor 1 Alters Monoaminergic Neurotransmission and Decreases Sensitivity to Amphetamine
- Biology, PsychologyNeuropsychopharmacology
- 2012
Overall, these data show that Taar1 brain overexpression causes hyposensitivity to amphetamine and alterations of monoaminergic neurotransmission and suggest that in vivo the receptor is either constitutively active and/or tonically activated by ambient levels of endogenous agonist(s).
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- BiologyFront. Neurosci.
- 2016
TAAR1 is uniquely positioned to exert direct control over DA and 5-HT neuronal firing and release, which has profound implications for understanding the pathophysiology of, and therefore designing more efficacious therapeutic interventions for, a range of neuropsychiatric disorders that involve aminergic dysregulation.
The Role of Biogenic Amine Transporters in Trace Amine–Associated Receptor 1 Regulation of Methamphetamine-Induced Neurotoxicity
- BiologyThe Journal of Pharmacology and Experimental Therapeutics
- 2019
It is demonstrated that a functional TAAR1 protects a specific subcellular fraction of VMAT2, but not the dopamine transporter, from methamphetamine-induced effects, suggesting new directions in pharmacotherapeutic development for neurodegenerative disorders.
A Receptor Mechanism for Methamphetamine Action in Dopamine Transporter Regulation in Brain
- Biology, ChemistryJournal of Pharmacology and Experimental Therapeutics
- 2009
Findings demonstrate a mediatory role of TAAR1 in methamphetamine action in DAT regulation and implicate this receptor as a potential target of therapeutics drugs for methamphetamine addiction.
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Differential Modulation of Beta-Adrenergic Receptor Signaling by Trace Amine-Associated Receptor 1 Agonists
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- 2011
Molecular details of TAAR1-ligand promiscuity are pointed to and specific trace amines are identified as allosteric or orthosteric ligands of particular β-adrenergic receptor subtypes are identified.
The Trace Amine-Associated Receptor 1 Agonist 3-Iodothyronamine Induces Biased Signaling at the Serotonin 1b Receptor
- BiologyFront. Pharmacol.
- 2018
Evidence is found for 5-HT1b as a new receptor target for 3-T1AM, albeit with a different signaling effect than the endogenous ligand, and a complex interrelation of signaling effects between the investigated GPCRs and respective ligands.
The Case for TAAR1 as a Modulator of Central Nervous System Function
- BiologyFront. Pharmacol.
- 2018
The bulk of evidence points to a significant physiological role of TAAR1 in the modulation of central nervous system function and a potential pharmacological role ofTAAR1 agonists in neurology and/or psychiatry, but many crucial issues require further investigation.
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