Abstract
The hypofunction hypothesis of glutamatergic neurotransmission via N-methyl-D-aspartate (NMDA) receptors in the pathophysiology of schizophrenia suggests that increasing NMDA receptor function via pharmacological manipulation could provide a new therapeutic strategy for schizophrenia. The glycine modulatory site on NMDA receptor complex is the one of the most attractive therapeutic targets for schizophrenia. One means of enhancing NMDA receptor neurotransmission is to increase the availability of the obligatory co-agonist glycine at modulatory site on the NMDA receptors through the inhibition of glycine transporter-1 (GlyT-1) on glial cells. Some clinical studies have demonstrated that the GlyT-1 inhibitor sarcosine (N-methylglycine) shows antipsychotic activity in patients with schizophrenia. Currently, a number of pharmaceutical companies have been developing novel and selective GlyT-1 inhibitors for the treatment of schizophrenia. A recent double blind phase II study demonstrated that the novel GlyT-1 inhibitor RG1678 has a robust and clinically meaningful effect in patients with schizophrenia. In this article, the author reviews the recent findings on the GlyT-1 as a potential therapeutic target of schizophrenia.
Keywords: Schizophrenia, NMDA receptor, Glutamate, Glycine, Transporter, Glia
Current Pharmaceutical Design
Title: Glycine Transporter-1: A New Potential Therapeutic Target for Schizophrenia
Volume: 17 Issue: 2
Author(s): Kenji Hashimoto
Affiliation:
Keywords: Schizophrenia, NMDA receptor, Glutamate, Glycine, Transporter, Glia
Abstract: The hypofunction hypothesis of glutamatergic neurotransmission via N-methyl-D-aspartate (NMDA) receptors in the pathophysiology of schizophrenia suggests that increasing NMDA receptor function via pharmacological manipulation could provide a new therapeutic strategy for schizophrenia. The glycine modulatory site on NMDA receptor complex is the one of the most attractive therapeutic targets for schizophrenia. One means of enhancing NMDA receptor neurotransmission is to increase the availability of the obligatory co-agonist glycine at modulatory site on the NMDA receptors through the inhibition of glycine transporter-1 (GlyT-1) on glial cells. Some clinical studies have demonstrated that the GlyT-1 inhibitor sarcosine (N-methylglycine) shows antipsychotic activity in patients with schizophrenia. Currently, a number of pharmaceutical companies have been developing novel and selective GlyT-1 inhibitors for the treatment of schizophrenia. A recent double blind phase II study demonstrated that the novel GlyT-1 inhibitor RG1678 has a robust and clinically meaningful effect in patients with schizophrenia. In this article, the author reviews the recent findings on the GlyT-1 as a potential therapeutic target of schizophrenia.
Export Options
About this article
Cite this article as:
Hashimoto Kenji, Glycine Transporter-1: A New Potential Therapeutic Target for Schizophrenia, Current Pharmaceutical Design 2011; 17 (2) . https://dx.doi.org/10.2174/138161211795049598
DOI https://dx.doi.org/10.2174/138161211795049598 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Synthesis of Bicyclic Aryl Thiazolines with Selective Anti-Proliferative Effects on Human Cancer Cell Lines
Letters in Organic Chemistry Neurotensin NTS1-Dopamine D2 Receptor-Receptor Interactions in Putative Receptor Heteromers: Relevance for Parkinson`s Disease and Schizophrenia
Current Protein & Peptide Science Nanoparticle Albumin - Bound (NAB) Technology is a Promising Method for Anti-Cancer Drug Delivery
Recent Patents on Anti-Cancer Drug Discovery Effects of Tea Polyphenols and their Polymers on MAPK Signaling Pathways in Cancer Research
Mini-Reviews in Medicinal Chemistry Biological Rationale for Regular Physical Exercise as an Effective Intervention for the Prevention and Treatment of Depressive Disorders
Current Pharmaceutical Design Dietary Polyphenols for Prostate Cancer Therapy
Current Bioactive Compounds Preclinical and Clinical Studies of Chidamide (CS055/HBI-8000), An Orally Available Subtype-selective HDAC Inhibitor for Cancer Therapy
Anti-Cancer Agents in Medicinal Chemistry Organosulfur Compounds in Cancer Chemoprevention
Mini-Reviews in Medicinal Chemistry Increased Paternal Age and Child Health and Development
Current Pediatric Reviews uPAR as Anti-Cancer Target: Evaluation of Biomarker Potential, Histological Localization, and Antibody-Based Therapy
Current Drug Targets Exploiting Endogenous Cellular Process to Generate Quinone Methides In Vivo
Current Organic Chemistry The Effects of Dietary Factors on the Androgen Receptor and Related Cellular Factors in Prostate Cancer
Current Medicinal Chemistry Diphenylpentane Skeleton as a Multi-Template for Steroid Skeleton- Recognizing Receptors/Enzymes
Mini-Reviews in Medicinal Chemistry Human Carbonyl Reductases
Current Drug Metabolism The Role of Mass Spectrometry in the “Omics” Era
Current Organic Chemistry Insulin Delivery Systems for Controlling Diabetes
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Signal Transduction and Heavy Ion Radiation Therapy: Biological Mechanisms, Biological Quality Assurance, and New Multimodality Approach
Current Signal Transduction Therapy iPSCs Derived from Malignant Tumor Cells: Potential Application for Cancer Research
Current Stem Cell Research & Therapy Gemini Surfactant Based Carriers in Gene and Drug Delivery
Current Medicinal Chemistry The Role of Fibroblast Growth Factors in Tumor Growth
Current Cancer Drug Targets