Abstract
A combination of pharmacological and genetic studies in mice confirmed that the Y1 and Y5 receptors mediate the potent orexigenic actions of exogenous NPY. Although the physiological role of NPY in causing obesity is less clear, potent and selective antagonists of both Y1 and Y5 have been developed. Some of the NPY antagonists have suitable pharmokinetic (PK) properties that allowed them to be evaluated in various rodent models of obesity. Several different Y1 and Y5 antagonists cause weight loss in rodent models, though confirmation that these effects are mechanism based has been limited. One Y5 antagonist, MK-0557 was evaluated in a 1-yr clinical trial and found to cause modest weight loss. Optimal NPY antagonist therapeutics for obesity may require blockade of both the Y1 and Y5 receptors.
Keywords: Neuropeptide Y, Y1, Y5, receptor, antagonist, obesity
Current Topics in Medicinal Chemistry
Title: NPY Y1 and Y5 Receptor Selective Antagonists as Anti-Obesity Drugs
Volume: 7 Issue: 17
Author(s): Douglas J. MacNeil
Affiliation:
Keywords: Neuropeptide Y, Y1, Y5, receptor, antagonist, obesity
Abstract: A combination of pharmacological and genetic studies in mice confirmed that the Y1 and Y5 receptors mediate the potent orexigenic actions of exogenous NPY. Although the physiological role of NPY in causing obesity is less clear, potent and selective antagonists of both Y1 and Y5 have been developed. Some of the NPY antagonists have suitable pharmokinetic (PK) properties that allowed them to be evaluated in various rodent models of obesity. Several different Y1 and Y5 antagonists cause weight loss in rodent models, though confirmation that these effects are mechanism based has been limited. One Y5 antagonist, MK-0557 was evaluated in a 1-yr clinical trial and found to cause modest weight loss. Optimal NPY antagonist therapeutics for obesity may require blockade of both the Y1 and Y5 receptors.
Export Options
About this article
Cite this article as:
MacNeil J. Douglas, NPY Y1 and Y5 Receptor Selective Antagonists as Anti-Obesity Drugs, Current Topics in Medicinal Chemistry 2007; 7 (17) . https://dx.doi.org/10.2174/156802607782341028
DOI https://dx.doi.org/10.2174/156802607782341028 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...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
-
Coronary Pressure Measurement Based Decision Making for Percutaneous Coronary Intervention
Current Cardiology Reviews Involvement of the Toxic AGEs (TAGE)-RAGE System in the Pathogenesis of Diabetic Vascular Complications: A Novel Therapeutic Strategy
Current Drug Targets Significance of Pharmacogenetics and Pharmacogenomics Research in Current Medical Practice
Current Drug Metabolism Cardiac Cell Therapy and Bypass Surgery
Current Pharmaceutical Design Evaluation of in-vitro Anti Diabetic Activity of a Siddha Herbo- Mineral Drug
Current Traditional Medicine Cancer Chemoprevention by Targeting the Epigenome
Current Drug Targets Pharmacologic Role of Vitamin D Natural Products
Current Vascular Pharmacology There is no Failure, Only Discovery—the Year Ahead for CARving New Paths
Current Alzheimer Research Nutraceuticals, A New Challenge for Medicinal Chemistry
Current Medicinal Chemistry Deep Inspiration Breath-hold (DIBH) Technique to Reduce Cardiac Radiation Dose in the Management of Breast Cancer
Current Cancer Therapy Reviews Homocysteine, Intracellular Signaling and Thrombotic Disorders
Current Medicinal Chemistry Disrupted White Matter Networks from Subjective Memory Impairment to Amnestic Mild Cognitive Impairment
Current Alzheimer Research Atheroma Burden and Morphology in Women
Current Pharmaceutical Design Modulation of MMP-9 Pathway by Lycopene in Macrophages and Fibroblasts Exposed to Cigarette Smoke
Inflammation & Allergy - Drug Targets (Discontinued) Biologics and the Cardiovascular System: A Double-Edged Sword
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Duration of Dual Antiplatelet Therapy After Coronary Stenting
Current Pharmaceutical Design Inflammatory Mechanisms in Atherosclerosis: The Impact of Matrix Metalloproteinases
Current Topics in Medicinal Chemistry Intestinal Barrier Dysfunction in Human Pathology and Aging
Current Pharmaceutical Design From Bone Marrow to Cardiac Atrial Appendage Stem Cells for Cardiac Repair: A Review
Current Medicinal Chemistry Giant Pulmonary Artery Aneurysm Secondary To Patent Ductus Arteriosus: A Case Report
Current Cardiology Reviews