ArticleProceedings of the National Academy of Sciences of the United States of America2011
TAAR1 activation modulates monoaminergic neurotransmission, preventing hyperdopaminergic and hypoglutamatergic activity.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 190 papers, 2 of them syntheses that pooled it.
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Who cites it
190 citing papers in PubMed, 2 syntheses or guidelines pooled it, 362 citations in OpenAlex.
- Trajectory of efficacy and safety across ulotaront dose levels in schizophrenia: a systematic review and dose-response meta-analysis.The international journal of neuropsychopharmacology · 2025Pooled it
- Trace amine-associated receptor 1 (TAAR1) agonism for psychosis: a living systematic review and meta-analysis of human and non-human data.Wellcome open research · 2024Pooled it
- Effect of TAAR1/5-HTTranslational psychiatry · 2021Trial
- Antipsychotic-like effects of TAAR1 agonists and D2 receptor blockers are mediated through distinct modulation of striatal neuronal dynamics.Molecular psychiatry · 2026Article
- Structure based discovery of antipsychotic-like TAAR1 agonists.Nature communications · 2026Article
- Novel selective morpholine trace amine-associated receptor 1 partial agonists show promising preclinical effects for neuropsychiatric disorders and are well tolerated in healthy volunteers.Molecular psychiatry · 2026Article
- Novel drug treatments for schizophrenia.Nature reviews. Drug discovery · 2026Review
- The 4-alkyl chain length of 2,5-dimethoxyamphetamines differentially affects in vitro serotonin receptor actions versus in vivo psychedelic-like effects.Molecular psychiatry · 2026Article
- New Pharmacological Treatment Approaches for Schizophrenia: Navigating the Post-iclepertin Landscape.CNS drugs · 2026Review
- Preclinical development of [European journal of nuclear medicine and molecular imaging · 2026Article
- The Role of Trace Amine-Associated Receptor 1 (TAAR1) in the Pathophysiology and Treatment of Depression.Current neuropharmacology · 2026Review
- TAAR1-mediated pathways regulating nigrostriatal function and the discovery and pharmacological characterization of a novel TAAR1 agonist, Selutaront.Frontiers in pharmacology · 2026Article
- TAAR1 deficiency impairs mitochondrial dynamics and synaptic integrity in the medial prefrontal cortex and associated cognition in mice.Translational psychiatry · 2025Article
- The role of the primary cilium in thyroid function and dysfunction with implications for thyroid disease.Histochemistry and cell biology · 2025Review
- Somatic Mosaicism Patterns Define Clinical-Surgical Subtypes of Focal Cortical Dysplasia Through Cell-Type-Specific Expression.medRxiv : the preprint server for health sciences · 2025Article
- Trace Amine-associated Receptors (TAARs): Candidate Targets in the Treatment of Bipolar Disorders.Actas espanolas de psiquiatria · 2025Review
- Trace amine-associated receptor 1 agonists differentially regulate dopamine transporter function.Molecular pharmacology · 2025Article
- Role of Glial Trace Amine Associated Receptor 1 (TAAR1) and Microbiota in Schizophrenia.Neurochemical research · 2025Review
- TAAR8 in the Brain: Implications for Dopaminergic Function, Neurogenesis, and Behavior.Biomedicines · 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
130 more citing papers are in PubMed but not listed here.
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Authors and funding
19 authors at 5 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The trace amine-associated receptor 1 (TAAR1), activated by endogenous metabolites of amino acids like the trace amines p-tyramine and β-phenylethylamine, has proven to be an important modulator of the dopaminergic system and is considered a promising target for the treatment of neuropsychiatric disorders. To decipher the brain functions of TAAR1, a selective TAAR1 agonist, RO5166017, was engineered. RO5166017 showed high affinity and potent functional activity at mouse, rat, cynomolgus monkey, and human TAAR1 stably expressed in HEK293 cells as well as high selectivity vs. other targets. In mouse brain slices, RO5166017 inhibited the firing frequency of dopaminergic and serotonergic neurons in regions where Taar1 is expressed (i.e., the ventral tegmental area and dorsal raphe nucleus, respectively). In contrast, RO5166017 did not change the firing frequency of noradrenergic neurons in the locus coeruleus, an area devoid of Taar1 expression. Furthermore, modulation of TAAR1 activity altered the desensitization rate and agonist potency at 5-HT(1A) receptors in the dorsal raphe, suggesting that TAAR1 modulates not only dopaminergic but also serotonergic neurotransmission. In WT but not Taar1(-/-) mice, RO5166017 prevented stress-induced hyperthermia and blocked dopamine-dependent hyperlocomotion in cocaine-treated and dopamine transporter knockout mice as well as hyperactivity induced by an NMDA antagonist. These results tie TAAR1 to the control of monoamine-driven behaviors and suggest anxiolytic- and antipsychotic-like properties for agonists such as RO5166017, opening treatment opportunities for psychiatric disorders.
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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.