Abstract
The role that the tridecapeptide neurotensin (NT) plays in the modulation of the aminoacidergic transmission is analyzed in different rat brain regions. NT exerts its effects through the activation of different receptor subtypes, NTR1, NTR2 and NTR3. The contribution of NTR1 receptor in modulating and reinforcing glutamate signalling will be shown including the involvement of interactions between NT and N-methyl-D-aspartate (NMDA) receptors. Extracellular accumulation of glutamate and the excessive activation of glutamate receptors, in particular NMDA receptors, is known to represent an important factor in the induction of glutamate-mediated neuronal damage occurring in Parkinsons disease and in pathologic events such as hypoxia and ischemia. An enhancing action of NT on glutamate-induced neurodegenerative effects is shown and NTR1 receptor antagonists could therefore become novel pharmaceutics in the treatment of neurodegenerative disease.
Keywords: Glutamate release, Glutamate-induced excitotoxicity, NMDA receptors, NTR1, Neurotensin receptor agonists and antagonists
Mini-Reviews in Medicinal Chemistry
Title: Emerging Evidence for Neurotensin Receptor 1 Antagonists as Novel Pharmaceutics in Neurodegenerative Disorders
Volume: 9 Issue: 12
Author(s): L. Ferraro, M. C. Tomasini, S. Beggiato, R. Guerrini, S. Salvadori, K. Fuxe, L. Calza, S. Tanganelli and T. Antonelli
Affiliation:
Keywords: Glutamate release, Glutamate-induced excitotoxicity, NMDA receptors, NTR1, Neurotensin receptor agonists and antagonists
Abstract: The role that the tridecapeptide neurotensin (NT) plays in the modulation of the aminoacidergic transmission is analyzed in different rat brain regions. NT exerts its effects through the activation of different receptor subtypes, NTR1, NTR2 and NTR3. The contribution of NTR1 receptor in modulating and reinforcing glutamate signalling will be shown including the involvement of interactions between NT and N-methyl-D-aspartate (NMDA) receptors. Extracellular accumulation of glutamate and the excessive activation of glutamate receptors, in particular NMDA receptors, is known to represent an important factor in the induction of glutamate-mediated neuronal damage occurring in Parkinsons disease and in pathologic events such as hypoxia and ischemia. An enhancing action of NT on glutamate-induced neurodegenerative effects is shown and NTR1 receptor antagonists could therefore become novel pharmaceutics in the treatment of neurodegenerative disease.
Export Options
About this article
Cite this article as:
Ferraro L., Tomasini C. M., Beggiato S., Guerrini R., Salvadori S., Fuxe K., Calza L., Tanganelli S. and Antonelli T., Emerging Evidence for Neurotensin Receptor 1 Antagonists as Novel Pharmaceutics in Neurodegenerative Disorders, Mini-Reviews in Medicinal Chemistry 2009; 9 (12) . https://dx.doi.org/10.2174/138955709789957495
DOI https://dx.doi.org/10.2174/138955709789957495 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Mitochondria as a Therapeutic Target in Metabolic Disorders
Mitochondria are the primary site of adenosine triphosphate (ATP) production in mammalian cells. Moreover, these organelles are an important source of reactive oxygen and nitrogen species in virtually any nucleated cell type. The modulation of a myriad of cellular signaling pathways depends on the mitochondrial physiology. Mitochondrial dysfunction is observed ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...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
Related Articles
-
Recent Advances in Characterizing Natural Products that Regulate Autophagy
Anti-Cancer Agents in Medicinal Chemistry Endoplasmic Reticulum Protein Quality Control in Neurodegenerative Disease: The Good, the Bad and the Therapy
Current Medicinal Chemistry Primary Progressive Aphasia-Defining Genetic and Pathological Subtypes
Current Alzheimer Research The Impact of Small Heat Shock Proteins (HspBs) in Alzheimer’s and Other Neurological Diseases
Current Pharmaceutical Design Thrombin: A Potential Proinflammatory Mediator in Neurotrauma and Neurodegenerative Disorders
Current Drug Targets - Inflammation & Allergy Multimodality Imaging of CXCR4 in Cancer: Current Status towards Clinical Translation
Current Molecular Medicine Phytocannabinoids and Cannabimimetic Drugs: Recent Patents in Central Nervous System Disorders
Recent Patents on CNS Drug Discovery (Discontinued) The Peripheral Anionic Site of Acetylcholinesterase: Structure, Functions and Potential Role in Rational Drug Design
Current Pharmaceutical Design Multi-Target-Directed Ligands Affecting Serotonergic Neurotransmission for Alzheimer’s Disease Therapy: Advances in Chemical and Biological Research
Current Medicinal Chemistry Drug Therapy of Neuropathic Pain: Current Developments and Future Perspectives
Current Drug Targets Patent Selections:
Recent Patents on CNS Drug Discovery (Discontinued) The Challenges in Moving from Ageing to Successful Longevity
Current Vascular Pharmacology Co-Enzyme Q10 to Treat Neurological Disorders: Basic Mechanisms, Clinical Outcomes, and Future Research Direction
CNS & Neurological Disorders - Drug Targets Reactive Astrocytes as Potential Manipulation Targets in Novel Cell Replacement Therapy of Parkinsons Disease
Current Drug Targets Phytochemicals for Drug Discovery in Alzheimer’s Disease: <i>In Silico</i> Advances
Current Pharmaceutical Design Calpain Inhibition: A Therapeutic Strategy Targeting Multiple Disease States
Current Pharmaceutical Design Functional Roles of Synaptic and Extrasynaptic NMDA Receptors in Physiological and Pathological Neuronal Activities
Current Drug Targets The Putative Use of Lithium in Alzheimer’s Disease
Current Alzheimer Research The Role of β-Amyloid Protein in Synaptic Function: Implications for Alzheimers Disease Therapy
Current Neuropharmacology Tau in Alzheimer Disease and Related Tauopathies
Current Alzheimer Research