Abstract
Neuropeptide Y (NPY) is present in the hypothalamus, where it is believed to play a key role in the control of food intake. Evidence for this assertion has come from studies demonstrating that acute administration of NPY into the hypothalamus or into the brain ventricles leads to increased food intake. In the case of chronic administration, the hyperphagic effects of NPY are prolonged leading to the development of an obese state. NPY levels in the hypothalamus are temporally correlated with food intake and are markedly elevated in response to energy depletion. However, attempts to demonstrate an important role for NPY in the control of food intake using NPY knockout mice, NPY antisense oligodeoxynucleotides and anti-NPY antibodies has produced equivocal results. Despite this many pharmaceutical companies have moved ahead with the search for agonists and antagonists of NPY receptor subtypes as antiobesity agents. Antagonists of the NPY Y1 and NPY Y5 receptor subtype initially looked promising since analogs of NPY with high selectivity for these receptors strongly stimulated food intake. However, attempts to inhibit the signaling of NPY through the NPY Y1 and NPY Y5 receptors has produced equivocal effects on food intake. Recent observations that the gut derived peptide PYY3-36 suppresses appetite by stimulating both peripherally and centrally located NPY Y2 receptors remain controversial in animals but the effects look promising in human studies. Whether this will be the long awaited therapy based on manipulation of NPY receptors will await further studies of long term efficacy and more importantly a favorable side effect profile.
Keywords: Neuropeptide Y, 1871-5273, PYY3-36, NPY receptors, NPY antagonists, NPY agonists
CNS & Neurological Disorders - Drug Targets
Title: NPY Receptors as Drug Targets for the Central Regulation of Body Weight
Volume: 5 Issue: 3
Author(s): Michel Feletou, Jean-Pierre Galizzi and Nigel R. Levens
Affiliation:
Keywords: Neuropeptide Y, 1871-5273, PYY3-36, NPY receptors, NPY antagonists, NPY agonists
Abstract: Neuropeptide Y (NPY) is present in the hypothalamus, where it is believed to play a key role in the control of food intake. Evidence for this assertion has come from studies demonstrating that acute administration of NPY into the hypothalamus or into the brain ventricles leads to increased food intake. In the case of chronic administration, the hyperphagic effects of NPY are prolonged leading to the development of an obese state. NPY levels in the hypothalamus are temporally correlated with food intake and are markedly elevated in response to energy depletion. However, attempts to demonstrate an important role for NPY in the control of food intake using NPY knockout mice, NPY antisense oligodeoxynucleotides and anti-NPY antibodies has produced equivocal results. Despite this many pharmaceutical companies have moved ahead with the search for agonists and antagonists of NPY receptor subtypes as antiobesity agents. Antagonists of the NPY Y1 and NPY Y5 receptor subtype initially looked promising since analogs of NPY with high selectivity for these receptors strongly stimulated food intake. However, attempts to inhibit the signaling of NPY through the NPY Y1 and NPY Y5 receptors has produced equivocal effects on food intake. Recent observations that the gut derived peptide PYY3-36 suppresses appetite by stimulating both peripherally and centrally located NPY Y2 receptors remain controversial in animals but the effects look promising in human studies. Whether this will be the long awaited therapy based on manipulation of NPY receptors will await further studies of long term efficacy and more importantly a favorable side effect profile.
Export Options
About this article
Cite this article as:
Feletou Michel, Galizzi Jean-Pierre and Levens R. Nigel, NPY Receptors as Drug Targets for the Central Regulation of Body Weight, CNS & Neurological Disorders - Drug Targets 2006; 5 (3) . https://dx.doi.org/10.2174/187152706777452236
DOI https://dx.doi.org/10.2174/187152706777452236 |
Print ISSN 1871-5273 |
Publisher Name Bentham Science Publisher |
Online ISSN 1996-3181 |
Call for Papers in Thematic Issues
Diagnosis and treatment of central nervous system infectious diseases
Infectious diseases of the central nervous system (CNS) can be divided into bacterial, tuberculous, viral, fungal, parasitic infections, etc. Early etiological treatment is often the most crucial means to reduce the mortality rate of patients with central nervous system infections, reduce complications and sequelae, and improve prognosis. The initial clinical ...read more
Techniques of Drug Repurposing: Delivering a new life to Herbs & Drugs
Of late, with the adaptation of innovative approaches and integration of advancements made towards medical sciences as well as the availability of a wide range of tools; several therapeutic challenges are being translated into viable clinical solutions, with a high degree of efficacy, safety, and selectivity. With a better understanding ...read more
Trends and perspectives in the rational management of CNS disorders
Central nervous system (CNS) diseases enforce a significant global health burden, driving ongoing efforts to improve our understanding and effectiveness of therapy. This issue investigates current advances in the discipline, focusing on the understanding as well as therapeutic handling of various CNS diseases. The issue covers a variety of diseases, ...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
-
Depression and Vascular Disease: Conceptual Issues, Relationships and Clinical Implications
Vascular Disease Prevention (Discontinued) Uptake and Metabolism of the Short-Chain Fatty Acid Butyrate, a Critical Review of the Literature
Current Drug Metabolism Current and Future Applications for Stem Cell Therapies in Spine Surgery
Current Stem Cell Research & Therapy Sleep, Depression and Insomnia – A Vicious Circle?
Current Psychiatry Reviews Recent Developments in Anti-dotes Against Anthrax
Recent Patents on Anti-Infective Drug Discovery Role of the Endocannabinoid System in the Neuroendocrine Responses to Inflammation
Current Pharmaceutical Design Cannabinoids and Neuro-Inflammation: Regulation of Brain Immune Response
Recent Patents on CNS Drug Discovery (Discontinued) HIV-1 Vpr: A Closer Look at the Multifunctional Protein from the Structural Perspective
Current HIV Research Multiligand Endocytosis and Congenital Defects: Roles of Cubilin, Megalin and Amnionless
Current Pharmaceutical Design The Role of Trophoblast Nutrient and Ion Transporters in the Development of Pregnancy Complications and Adult Disease
Current Vascular Pharmacology Tissue Distribution and Pharmacodynamics: A Complicated Relationship
Current Drug Metabolism DNAJ Proteins and Protein Aggregation Diseases
Current Topics in Medicinal Chemistry Gender Bias in Acute Coronary Syndromes
Current Vascular Pharmacology Improving the Stability of Aptamers by Chemical Modification
Current Medicinal Chemistry Current Drug Targets for Antihyperlipidemic Therapy
Mini-Reviews in Medicinal Chemistry Epidemiology and Risk Factors of Cerebral Ischemia and Ischemic Heart Diseases: Similarities and Differences
Current Cardiology Reviews Genome-Wide Association Studies: Is there a Genotype for Cognitive Decline in Older Persons with Type 2 Diabetes?
Current Pharmaceutical Design Cytopathological Mechanisms in Mitochondrial Disease
Current Chemical Biology The Stroke-Induced Blood-Brain Barrier Disruption: Current Progress of Inspection Technique, Mechanism, and Therapeutic Target
Current Neuropharmacology Progress and Outlooks in a Genetic Absence Epilepsy Model (WAG/Rij)
Current Medicinal Chemistry