ArticleThe international journal of neuropsychopharmacology2023
In Vitro Comparison of Ulotaront (SEP-363856) and Ralmitaront (RO6889450): Two TAAR1 Agonist Candidate Antipsychotics.
Article in The international journal of neuropsychopharmacology, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 19 citations in OpenAlex.
- Antipsychotic-like effects of TAAR1 agonists and D2 receptor blockers are mediated through distinct modulation of striatal neuronal dynamics.Molecular psychiatry · 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
- Towards Mechanism-Informed Treatments for Mental Health.Journal of neurochemistry · 2026Review
- Esflurbiprofen exerts a fast-onset antidepressant effect by blocking SERT-nNOS interaction.Acta pharmacologica Sinica · 2026Article
- New Pharmacological Treatment Approaches for Schizophrenia: Navigating the Post-iclepertin Landscape.CNS drugs · 2026Review
- TAAR1-mediated pathways regulating nigrostriatal function and the discovery and pharmacological characterization of a novel TAAR1 agonist, Selutaront.Frontiers in pharmacology · 2026Article
- Beyond dopamine: KarXT and emerging mechanism-based therapies in schizophrenia.Frontiers in psychiatry · 2026Review
- Estimation of Dopamine DACS chemical neuroscience · 2025Article
- New pharmacological approaches in the treatment of schizophrenia.Pharmacological reports : PR · 2025Review
- Trace amine-associated receptor 1 (TAAR1): an emerging therapeutic target for neurodegenerative, neurodevelopmental, and neurotraumatic disorders.Naunyn-Schmiedeberg's archives of pharmacology · 2025Review
- Overview of Novel Antipsychotic Drugs: State of the Art, New Mechanisms, and Clinical Aspects of Promising Compounds.Biomedicines · 2025Review
- AlphaFold accelerated discovery of psychotropic agonists targeting the trace amine-associated receptor 1.Science advances · 2024Article
- Computational Methods for the Discovery and Optimization of TAAR1 and TAAR5 Ligands.International journal of molecular sciences · 2024Review
- Elucidating the molecular pharmacology of trace amine-associated receptor 1 to advance antipsychotic drug discovery.Clinical and translational medicine · 2024Article
- Trace amine-associated receptors (TAARs)2-9 knockout mice exhibit reduced wakefulness and disrupted REM sleep.Frontiers in psychiatry · 2024Article
- TAAR1 as an emerging target for the treatment of psychiatric disorders.Pharmacology & therapeutics · 2024Review
- Discovery of Guanfacine as a Novel TAAR1 Agonist: A Combination Strategy through Molecular Modeling Studies and Biological Assays.Pharmaceuticals (Basel, Switzerland) · 2023Article
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundTrace amine-associated receptor-1 (TAAR1) agonists have been proposed as potential antipsychotics, with ulotaront and ralmitaront having reached clinical trials. While ulotaront demonstrated efficacy in a recent Phase II trial, a corresponding study studies of ralmitaront failed to show efficacy as a monotherapy or as an adjunct to atypical antipsychotics. In addition to TAAR1 agonism, ulotaront is a partial agonist at the serotonin 1A receptor (5-HT1AR). However, little is known about ralmitaront.
methodsWe compared ulotaront and ralmitaront at TAAR1, 5-HT1AR, and dopamine D2 using luciferase complementation-based G protein recruitment, cAMP accumulation, and G protein-coupled inward rectifier potassium channel activation assays.
resultsRalmitaront showed lower efficacy at TAAR1 in G protein recruitment, cAMP accumulation, and GIRK activation assays. Moreover, ralmitaront lacked detectable activity at 5-HT1AR and dopamine D2.
conclusionsCompared with ulotaront, ralmitaront shows lower efficacy and slower kinetics at TAAR1 and lacks efficacy at 5-HT1AR. These data may be relevant to understanding differences in clinical profiles of these 2 compounds.
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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 Socratic graph.