FTBMT, a Novel and Selective GPR52 Agonist, Demonstrates Antipsychotic-Like and Procognitive Effects in Rodents, Revealing a Potential Therapeutic Agent for Schizophrenia

No abstract is available for this paper.

• Publication year

  2017

• Venue

  Journal of Pharmacology and Experimental Therapeutics

• Publication date

  2017-11-01

• Fields of study

  Medicine, Psychology

• Identifiers
  DOI 10.1124/jpet.117.242925PMID 28851764
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Design, synthesis, and pharmacological evaluation of 4-azolyl-benzamide derivatives as novel GPR52 agonists.

  2017cited by this paper
• The Phosphodiesterase 10A Selective Inhibitor TAK-063 Improves Cognitive Functions Associated with Schizophrenia in Rodent Models

  2016cited by this paper
• Temporal and Spatial Transcriptional Fingerprints by Antipsychotic or Propsychotic Drugs in Mouse Brain

  2015influential reference
• Antipsychotic treatment and functional connectivity of the striatum in first-episode schizophrenia.

  2015cited by this paper
• In Vivo Pharmacological Characterization of TAK-063, a Potent and Selective Phosphodiesterase 10A Inhibitor with Antipsychotic-Like Activity in Rodents

  2015cited by this paper
• Perspectives on the mGluR2/3 agonists as a therapeutic target for schizophrenia: Still promising or a dead end?

  2015cited by this paper
• Discovery of the first potent and orally available agonist of the orphan G-protein-coupled receptor 52.

  2014cited by this paper
• Anatomical Transcriptome of G Protein-Coupled Receptors Leads to the Identification of a Novel Therapeutic Candidate GPR52 for Psychiatric Disorders

  2014influential reference
• Schizophrenia drug gets negative results for negative symptoms

  2014cited by this paper
• Interplay of hippocampus and prefrontal cortex in memory.

  2013influential reference
• GABAergic interneuron origin of schizophrenia pathophysiology.

  2012cited by this paper
• Pharmacological treatment of schizophrenia: a critical review of the pharmacology and clinical effects of current and future therapeutic agents

  2012cited by this paper
• Animal models of schizophrenia

  2011influential reference
• Unique Antipsychotic Activities of the Selective Metabotropic Glutamate Receptor 1 Allosteric Antagonist 2-Cyclopropyl-5-[1-(2-fluoro-3-pyridinyl)-5-methyl-1H-1,2,3-triazol-4-yl]-2,3-dihydro-1H-isoindol-1-one

  2009influential reference
• Reality of auditory verbal hallucinations

  2009cited by this paper
• Using the MATRICS to guide development of a preclinical cognitive test battery for research in schizophrenia.

  2009cited by this paper
• Distinct Roles of PDE4 and PDE10A in the Regulation of cAMP/PKA Signaling in the Striatum

  2008cited by this paper
• Lurasidone reverses MK-801-induced impairment of learning and memory in the Morris water maze and radial-arm maze tests in rats.

  2008cited by this paper
• An update on adenosine A2A-dopamine D2 receptor interactions: implications for the function of G protein-coupled receptors.

  2008cited by this paper
• Anticataleptic 8-OH-DPAT preferentially counteracts with haloperidol-induced Fos expression in the dorsolateral striatum and the core region of the nucleus accumbens.

  2008cited by this paper
• Differential expression of IEG mRNA in rat brain following acute treatment with clozapine or haloperidol: a semi-quantitative RT—PCR study

  2008cited by this paper
• Dopamine D1 receptors regulate protein synthesis-dependent long-term recognition memory via extracellular signal-regulated kinase 1/2 in the prefrontal cortex.

  2007influential reference
• Object recognition in rats and mice: a one-trial non-matching-to-sample learning task to study 'recognition memory'

  2006cited by this paper
• Involvement of adenosine receptors in dizocilpine-induced motor activity in mice.

  2006cited by this paper
• Protein kinase A regulates calcium permeability of NMDA receptors

  2006cited by this paper
• Current schizophrenia drugs: efficacy and side effects

  2006cited by this paper
• A Systematic Review of the Prevalence of Schizophrenia

  2005cited by this paper
• The effects of ziprasidone on regional c-Fos expression in the rat forebrain

  2005cited by this paper
• Aspin–Welch Test

  2005cited by this paper
• Impaired delayed spatial win-shift behaviour on the eight arm radial maze following excitotoxic lesions of the medial prefrontal cortex in the rat.

  2003influential reference
• CREB, memory enhancement and the treatment of memory disorders: promises, pitfalls and prospects

  2003cited by this paper
• The mouse brain in stereotaxic coordinates

  2003cited by this paper
• Presynaptic adenosine A2A receptors enhance GABAergic synaptic transmission via a cyclic AMP dependent mechanism in the rat globus pallidus

  2002cited by this paper
• The emerging role of glutamate in the pathophysiology and treatment of schizophrenia.

  2001cited by this paper
• Relationship between symptom dimensions and neurocognitive functioning in schizophrenia: a meta-analysis of WCST and CPT studies. Wisconsin Card Sorting Test. Continuous Performance Test.

  2001cited by this paper
• GABAergic involvement in motor effects of an adenosine A(2A) receptor agonist in mice.

  2000cited by this paper
• Impaired Recognition Memory in Rats after Damage to the Hippocampus

  2000cited by this paper
• Preferential inhibition of dizocilpine-induced hyperlocomotion by olanzapine.

  1999cited by this paper
• Beyond the dopamine receptor: the DARPP-32/protein phosphatase-1 cascade.

  1999cited by this paper
• Identification and cloning of three novel human G protein-coupled receptor genes GPR52, PsiGPR53 and GPR55: GPR55 is extensively expressed in human brain.

  1999influential reference
• The Role of Serotonin in Antipsychotic Drug Action

  1999cited by this paper
• Reciprocal interactions between adenosine A2A and dopamine D2 receptors in Chinese hamster ovary cells co-transfected with the two receptors.

  1999cited by this paper
• Mesolimbic Activity Associated with Psychosis in Schizophrenia: Symptom‐specific PET Studies

  1999cited by this paper
• Comparison of dopamine receptor antagonists on hyperlocomotion induced by cocaine, amphetamine, MK-801 and the dopamine D1 agonist C-APB in mice

  1999cited by this paper
• Sigma receptor ligands (+)-SKF10,047 and SA4503 improve dizocilpine-induced spatial memory deficits in rats.

  1998cited by this paper
• Adenosine A2A receptor agonists increase Fos-like immunoreactivity in mesolimbic areas.

  1997cited by this paper
• Adenosine A2A Agonists: A Potential New Type of Atypical Antipsychotic

  1997cited by this paper
• Reserpine: A tragic victim of myths, marketing, and fashionable prescribing

  1996cited by this paper
• Acute administration of typical and atypical antipsychotic drugs induces distinctive patterns of Fos expression in the rat forebrain.

  1995cited by this paper
• Differential expression of c-fos and zif268 in rat striatum after haloperidol, clozapine, and amphetamine.

  1992cited by this paper
• A non-parametric equivalent of Williams' test for contrasting increasing dose levels of a treatment.

  1977cited by this paper
• A test for differences between treatment means when several dose levels are compared with a zero dose control.

  1971cited by this paper
• A test for differences between treatment means when several dose levels are compared with a zero dose control.

  1971cited by this paper
• STATISTICAL METHODS

  1967cited by this paper
• Behavioral Neuroscience

  year unknowncited by this paper

• Targeting GPR52 for potential agonists for schizophrenia therapy: A computational drug discovery study.

  2025cites this paper
• Constitutive activity among orphan G protein-coupled receptors: Molecular mechanisms and pharmacological perspectives.

  2025cites this paper
• Class A Orphans in GtoPdb v.2025.4

  2025cites this paper
• Orphan GPR52 as an emerging neurotherapeutic target.

  2024cites this paper
• The Orphan G Protein-Coupled Receptor GPR52 is a Novel Regulator of Breast Cancer Multicellular Organization

  2024cites this paper
• Exploring orphan GPCRs in neurodegenerative diseases

  2024cites this paper
• Discovery of 3-((4-Benzylpyridin-2-yl)amino)benzamides as Potent GPR52 G Protein-Biased Agonists.

  2024cites this paper
• The Identification of GPR52 Agonist HTL0041178, a Potential Therapy for Schizophrenia and Related Psychiatric Disorders.

  2023cites this paper
• The non-nutritive sweetener sucralose increases β-arrestin signaling at the constitutively active orphan G protein-coupled receptor GPR52.

  2023cites this paper
• Dynamic Insights into the Self-Activation Pathway and Allosteric Regulation of the Orphan G-Protein-Coupled Receptor GPR52

  2023cites this paper
• Molecular insights into orphan G protein‐coupled receptors relevant to schizophrenia

  2023influential citation
• G protein-coupled receptors (GPCRs) as Potential Therapeutics for Psychiatric Disorders.

  2023cites this paper
• GPR52 regulates cAMP in T cells but is dispensable for encephalitogenic responses

  2023cites this paper
• Current Trends in the Animal Models for Screening of Nootropic Agents.

  2022cites this paper
• The effects and mechanism of environmental enrichment on MK-801 induced cognitive impairment in rodents with schizophrenia

  2022cites this paper
• Innovative Therapeutic Approaches for Huntington’s Disease: From Nucleic Acids to GPCR-Targeting Small Molecules

  2021cites this paper
• Characterisation of inverse agonism of the orphan-G protein-coupled receptor GPR52 by cannabinoid ligands Cannabidiol and O-1918

  2021cites this paper
• Targeted Proteomics Combined with Affinity Mass Spectrometry Analysis Reveals Antagonist E7 Acts As an Intracellular Covalent Ligand of Orphan Receptor GPR52.

  2020cites this paper
• Discovery of Potent and Brain-Penetrant GPR52 Agonist that Suppresses Psychostimulant Behavior.

  2020cites this paper
• Orphan G Protein Coupled Receptors in Affective Disorders

  2020cites this paper
• A β-arrestin-2-dependent mechanism of GPR52 signalling in frontal cortical neurons.

  2020cites this paper
• Translation-Focused Approaches to GPCR Drug Discovery for Cognitive Impairments Associated with Schizophrenia.

  2020cites this paper
• In the loop: extra-striatal regulation of spiny projection neurons by GPR52.

  2020cites this paper
• Structural basis of ligand recognition and self-activation of orphan GPR52

  2020cites this paper
• Tackling the complexities of orphan GPCR ligand discovery with rationally assisted approaches

  2020cites this paper
• Potential Utility of Biased GPCR Signaling for Treatment of Psychiatric Disorders

  2019cites this paper
• GLYX-13 Ameliorates Schizophrenia-Like Phenotype Induced by MK-801 in Mice: Role of Hippocampal NR2B and DISC1

  2018cites this paper
• Phosphodiesterase 2A Inhibitor TAK-915 Ameliorates Cognitive Impairments and Social Withdrawal in N-Methyl-d-Aspartate Receptor Antagonist–Induced Rat Models of Schizophrenia

  2018cites this paper
• Commentary: GLYX-13 Ameliorates Schizophrenia-Like Phenotype Induced by MK-801 in Mice: Role of Hippocampal NR2B and DISC1

  2018cites this paper
• Expression map of 78 brain-expressed mouse orphan GPCRs provides a translational resource for neuropsychiatric research

  2018cites this paper