ArticlePsychopharmacology2015
Functional profile of a novel modulator of serotonin, dopamine, and glutamate neurotransmission.
Article in Psychopharmacology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It is linked to trial NCT05890768 (The Relationship Between the Efficacy of Lumateperone and Central Glutamate and Dopaminergic Metabolism), which is not on this map. Cited by 45 papers, 4 of them syntheses that pooled it.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
The Relationship Between the Efficacy of Lumateperone and Central Glutamate and Dopaminergic Metabolism: A Comparison With Risperidone in First Episode Psychosis
Who cites it
45 citing papers in PubMed, 4 syntheses or guidelines pooled it, 281 citations in OpenAlex.
- Effect of dopamine partial agonist antipsychotics on suicide risk in persons with schizophrenia and schizoaffective disorders: A systematic review and meta-analysis.Schizophrenia research · 2026Pooled it
- Efficacy and safety of lumateperone for bipolar depression and schizophrenia: a systematic review and meta-analysis.The international journal of neuropsychopharmacology · 2024Pooled it
- Canonical and Non-Canonical Antipsychotics' Dopamine-Related Mechanisms of Present and Next Generation Molecules: A Systematic Review on Translational Highlights for Treatment Response and Treatment-Resistant Schizophrenia.International journal of molecular sciences · 2023Pooled it
- New Antipsychotic Medications in the Last Decade.Current psychiatry reports · 2021Pooled it
- Long-term safety and tolerability of lumateperone 42 mg in patients with bipolar disorder: results from a 6-month open-label extension study.International clinical psychopharmacology · 2026Trial
- Lumateperone monotherapy for major depressive episodes associated with bipolar disorder: efficacy and safety in a randomized placebo-controlled trial.International clinical psychopharmacology · 2026Trial
- Efficacy of Lumateperone in depression associated with bipolar II disorder: a pooled analysis of late-phase clinical trials.CNS spectrums · 2025Trial
- Efficacy and Safety of Lumateperone for Treatment of Schizophrenia: A Randomized Clinical Trial.JAMA psychiatry · 2020Trial
- Dopamine DNeuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2019Trial
- Lumateperone for the Treatment of Major Depressive Disorder With Mixed Features or Bipolar Depression With Mixed Features: A Randomized Placebo-Controlled Trial.Journal of clinical psychopharmacologyTrial
- Article
- Advances in the treatment of Alzheimer's disease.Frontiers in pharmacology · 2026Review
- Efficacy of Adjunctive Lumateperone 42 mg on Anhedonia and Across a Broad Range of Depressive Symptoms in Major Depressive Disorder: Post Hoc Analysis of a Phase 3, Randomized, Placebo-Controlled Trial.Neuropsychiatric disease and treatment · 2026Article
- Third-Generation Antipsychotics: The Quest for the Key to Neurotrophism.Life (Basel, Switzerland) · 2025Review
- Transforming Alzheimer's Treatment: Unveiling New Potential with Drug Repurposing Strategies.Current medicinal chemistry · 2025Review
- Exploring the Pharmacological and Clinical Features of Lumateperone: A Promising Novel Antipsychotic.International journal of molecular sciences · 2024Review
- Adverse event signal mining and severe adverse event influencing factor analysis of Lumateperone based on FAERS database.Frontiers in pharmacology · 2024Article
- Structure, function and drug discovery of GPCR signaling.Molecular biomedicine · 2023Review
- The Novel Antipsychotic Lumateperone (Iti-007) in the Treatment of Schizophrenia: A Systematic Review.Brain sciences · 2023Review
- A Review of the Characteristics of Clinical Trials and Potential Medications for Alcohol Dependence: Data Analysis from ClinicalTrials.gov.Medicina (Kaunas, Lithuania) · 2023Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
14 authors at 4 institutions in 2 countries.
Funding
Abstract
rationaleSchizophrenia remains among the most prevalent neuropsychiatric disorders, and current treatment options are accompanied by unwanted side effects. New treatments that better address core features of the disease with minimal side effects are needed.
objectivesAs a new therapeutic approach, 1-(4-fluoro-phenyl)-4-((6bR, 10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3',4':4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-butan-1-one (ITI-007) is currently in human clinical trials for the treatment of schizophrenia. Here, we characterize the preclinical functional activity of ITI-007.
resultsITI-007 is a potent 5-HT2A receptor ligand (K i = 0.5 nM) with strong affinity for dopamine (DA) D2 receptors (K i = 32 nM) and the serotonin transporter (SERT) (K i = 62 nM) but negligible binding to receptors (e.g., H1 histaminergic, 5-HT2C, and muscarinic) associated with cognitive and metabolic side effects of antipsychotic drugs. In vivo it is a 5-HT2A antagonist, blocking (±)-2,5-dimethoxy-4-iodoamphetamine hydrochloride (DOI)-induced headtwitch in mice with an inhibitory dose 50 (ID50) = 0.09 mg/kg, per oral (p.o.), and has dual properties at D2 receptors, acting as a postsynaptic D2 receptor antagonist to block D-amphetamine hydrochloride (D-AMPH) hyperlocomotion (ID50 = 0.95 mg/kg, p.o.), yet acting as a partial agonist at presynaptic striatal D2 receptors in assays measuring striatal DA neurotransmission. Further, in microdialysis studies, this compound significantly and preferentially enhances mesocortical DA release. At doses relevant for antipsychotic activity in rodents, ITI-007 has no demonstrable cataleptogenic activity. ITI-007 indirectly modulates glutamatergic neurotransmission by increasing phosphorylation of GluN2B-type N-methyl-D-aspartate (NMDA) receptors and preferentially increases phosphorylation of glycogen synthase kinase 3β (GSK-3β) in mesolimbic/mesocortical dopamine systems.
conclusionThe combination of in vitro and in vivo activities of this compound support its development for the treatment of schizophrenia and other psychiatric and neurologic disorders.
Indexed as
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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.