Abstract
Central nervous system (CNS) selective amino acid transporters provide an important function in maintaining tonic extracellular levels of amino acids that act as neurotransmitters, synaptic modulators or neurotransmitter precursors. Small molecule inhibitors of these transporters have been postulated and in some cases demonstrated to be useful in the treatment of a range of CNS driven disorders such as epilepsy, anxiety, psychosis, depre-ssion, pain and neurodegenerative disease. Although much of the research to date in this field has focussed on inhibition of the g -amino butyric acid (GABA) transporters more recent reports have also generated interest in modulation of glycine, glutamate and proline transporters. This article will review the current medicinal chemistry literature and structure activity relationships known for mammalian CNS selective amino acid transporters.
Keywords: inhibitors, mammalian central nervous system, amino butyric acid GABA transporters, GAT1, Glycine transporter, proline transporter, taurine transporter, cationic amino acid transporters, glutamate transporters
Current Medicinal Chemistry
Title: Inhibitors of Mammalian Central Nervous System Selective Amino Acid Transporters
Volume: 7 Issue: 2
Author(s): Richard E. Armer
Affiliation:
Keywords: inhibitors, mammalian central nervous system, amino butyric acid GABA transporters, GAT1, Glycine transporter, proline transporter, taurine transporter, cationic amino acid transporters, glutamate transporters
Abstract: Central nervous system (CNS) selective amino acid transporters provide an important function in maintaining tonic extracellular levels of amino acids that act as neurotransmitters, synaptic modulators or neurotransmitter precursors. Small molecule inhibitors of these transporters have been postulated and in some cases demonstrated to be useful in the treatment of a range of CNS driven disorders such as epilepsy, anxiety, psychosis, depre-ssion, pain and neurodegenerative disease. Although much of the research to date in this field has focussed on inhibition of the g -amino butyric acid (GABA) transporters more recent reports have also generated interest in modulation of glycine, glutamate and proline transporters. This article will review the current medicinal chemistry literature and structure activity relationships known for mammalian CNS selective amino acid transporters.
Export Options
About this article
Cite this article as:
Armer E. Richard, Inhibitors of Mammalian Central Nervous System Selective Amino Acid Transporters, Current Medicinal Chemistry 2000; 7 (2) . https://dx.doi.org/10.2174/0929867003375380
DOI https://dx.doi.org/10.2174/0929867003375380 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...read more
![](/images/wayfinder.jpg)
- 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
-
Susceptibility Genes for the Side Effect of Antipsychotics on Body Weight and Obesity
Current Drug Targets Novel 3-{4-[2-Amino-4-(Substitutedphenyl)-2H-[1, 3] Oxazin/Thiazin-6-Yl} -2-Phenyl-3H-Quinazolin-4-One Derivatives as Enhancer of GABA Mediated Inhibition: Synthesis, Molecular Modeling and Pharmacological Studies
Letters in Drug Design & Discovery Population-based Study of Risk Polymorphisms Associated with Vascular Disorders and Dementia
Current Genomics Editorial
Current Pediatric Reviews Synthesis and Biological Evaluation of New 4-Thiazolidinone Derivatives as Carbonic Anhydrase Inhibitors
Letters in Organic Chemistry Substituted Aminobenzothiazole Derivatives of Tacrine: Synthesis and Study on Learning and Memory Impairment in Scopolamine-Induced Model of Amnesia in Rat
Mini-Reviews in Medicinal Chemistry Derivatives of Deoxypodophyllotoxin Induce Apoptosis through Bcl-2/Bax Proteins Expression
Anti-Cancer Agents in Medicinal Chemistry Patent Selections:
Recent Patents on Regenerative Medicine Protein Kinases and their Modulation in the Central Nervous System
Current Medicinal Chemistry - Central Nervous System Agents Patent Annotations
Recent Patents on CNS Drug Discovery (Discontinued) Valproic acid, A Potential Inducer of Osteogenesis in Mouse Mesenchymal Stem Cells
Current Molecular Pharmacology Recent Development in Substituted Benzothiazole as an Anticonvulsant Agent
Mini-Reviews in Medicinal Chemistry Clinical Studies with Targeted Toxins in Malignant Glioma
Reviews on Recent Clinical Trials Natural Products as a Source of CNS-Active Agents
Mini-Reviews in Organic Chemistry The Use of <i>Cannabis</i> and Cannabinoid-based Products by Pregnant Women: A Patent Review
Recent Patents on Biotechnology Dry Age-Related Macular Degeneration: Recent Progress of Therapeutic approaches
Current Molecular Pharmacology Alpha-7 Nicotinic Receptors in Nervous System Disorders: From Function to Therapeutic Perspectives
Central Nervous System Agents in Medicinal Chemistry PET/MR Tomographs: A Review with Technical, Radiochemical and Clinical Perspectives
Current Radiopharmaceuticals Heterocyclic Compounds as Anti-Inflammatory Agents
Current Bioactive Compounds An Overview of EEG Seizure Detection Units and Identifying their Complexity- A Review
Current Signal Transduction Therapy