Abstract
Since Rimonabant was withdrawn in Europe in 2008 because of its substantial CNS risk factors including depression and anxiety, the development of anti-obesity drugs targeting CB1R in the brain has been suspended and/or terminated globally. Instead, developing peripherally restricted CB1R antagonists is actively pursued in the hope that not only could they eliminate any CNS adverse effects observed with Rimonabant, but also maintain therapeutic benefits in metabolic syndrome, including obesity, type 2 diabetes, and non-alcoholic fatty liver diseases. In this review, we summarized the most recent advances that have been made on this area, with particular emphasis on various synthetic approaches, whereby the increase in polarity, water solubility and polar surface area were centralized on, toward potential peripheralacting CB1 antagonists.
Keywords: Crossing the Blood-Brain Barrier, Metabolic disorders, Cannabinoid 1 receptor, Peripheral antagonists, SR141716A, CNS risk factors, depression, anxiety, anti-obesity drugs, antagonists, CNS adverse effects, metabolic syndrome, type 2 diabetes, non-alcoholic fatty liver diseases, water solubility, peripheralacting CB1 antagonists
Current Topics in Medicinal Chemistry
Title: A New Perspective of Cannabinoid 1 Receptor Antagonists: Approaches Toward Peripheral CB1R Blockers without Crossing the Blood-Brain Barrier
Volume: 11 Issue: 12
Author(s): Yen-Ku Wu, Ching-Fang Yeh, Tai Wei Ly and Ming-Shiu Hung
Affiliation:
Keywords: Crossing the Blood-Brain Barrier, Metabolic disorders, Cannabinoid 1 receptor, Peripheral antagonists, SR141716A, CNS risk factors, depression, anxiety, anti-obesity drugs, antagonists, CNS adverse effects, metabolic syndrome, type 2 diabetes, non-alcoholic fatty liver diseases, water solubility, peripheralacting CB1 antagonists
Abstract: Since Rimonabant was withdrawn in Europe in 2008 because of its substantial CNS risk factors including depression and anxiety, the development of anti-obesity drugs targeting CB1R in the brain has been suspended and/or terminated globally. Instead, developing peripherally restricted CB1R antagonists is actively pursued in the hope that not only could they eliminate any CNS adverse effects observed with Rimonabant, but also maintain therapeutic benefits in metabolic syndrome, including obesity, type 2 diabetes, and non-alcoholic fatty liver diseases. In this review, we summarized the most recent advances that have been made on this area, with particular emphasis on various synthetic approaches, whereby the increase in polarity, water solubility and polar surface area were centralized on, toward potential peripheralacting CB1 antagonists.
Export Options
About this article
Cite this article as:
Wu Yen-Ku, Yeh Ching-Fang, Wei Ly Tai and Hung Ming-Shiu, A New Perspective of Cannabinoid 1 Receptor Antagonists: Approaches Toward Peripheral CB1R Blockers without Crossing the Blood-Brain Barrier, Current Topics in Medicinal Chemistry 2011; 11 (12) . https://dx.doi.org/10.2174/156802611795860997
DOI https://dx.doi.org/10.2174/156802611795860997 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
AlphaFold in Medicinal Chemistry: Opportunities and Challenges
AlphaFold, a groundbreaking AI tool for protein structure prediction, is revolutionizing drug discovery. Its near-atomic accuracy unlocks new avenues for designing targeted drugs and performing efficient virtual screening. However, AlphaFold's static predictions lack the dynamic nature of proteins, crucial for understanding drug action. This is especially true for multi-domain proteins, ...read more
Artificial intelligence for Natural Products Discovery and Development
Our approach involves using computational methods to predict the potential therapeutic benefits of natural products by considering factors such as drug structure, targets, and interactions. We also employ multitarget analysis to understand the role of drug targets in disease pathways. We advocate for the use of artificial intelligence in predicting ...read more
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
- 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
-
Ezetimibe and Reactive Oxygen Species
Current Vascular Pharmacology Editorial (Thematic Issue: Pharmacologic Strategies with Afterload Reduction in Low Cardiac Output Syndrome After Pediatric Cardiac Surgery)
Current Vascular Pharmacology Casein Phosphopeptides in Oral Health - Chemistry and Clinical Applications
Current Pharmaceutical Design Evaluating 3D-printed Bolus Compared to Conventional Bolus Types Used in External Beam Radiation Therapy
Current Medical Imaging β-Adrenergic Over-Stimulation and Cardio-Myocyte Apoptosis: Two Receptors, One Organelle, Two Fates?
Current Drug Targets Serum Amyloid A and Its Potential Physiological / Pathological Functions - an Overview of Patents
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Metabolic Therapy of Heart Failure
Current Pharmaceutical Design The Double Roles of the Prostaglandin E<sub>2</sub> EP2 Receptor in Intracerebral Hemorrhage
Current Drug Targets Physiology of Folic Acid in Health and Disease
Current Drug Metabolism Artery of Percheron Infarction: A Characteristic Pattern of Ischemia and Variable Clinical Presentation: A Literature Review
Current Medical Imaging Cell Hierarchy, Metabolic Flexibility and Systems Approaches to Cancer Treatment
Current Pharmaceutical Biotechnology Clinical Significance of the New Cardiovascular Risk Markers in Diabetes Mellitus
Current Diabetes Reviews Benefits of SGLT2 Inhibitors Beyond Glycemic Control – A Focus on Metabolic, Cardiovascular and Renal Outcomes
Current Diabetes Reviews Atrial Remodeling and Novel Pharmacological Strategies for Antiarrhythmic Therapy in Atrial Fibrillation
Current Medicinal Chemistry Critical Roles of Insulin-Induced Senescence in Diabetic Vasculopathy
Vascular Disease Prevention (Discontinued) Relaxin Receptors - New Drug Targets for Multiple Disease States
Current Drug Targets Editorial (Thematic Issue: Measuring Myocyte Oxidative Stress and Targeting Cytokines to Evaluate Inflammatory Response and Cardiac Repair after Myocardial Infarction)
Current Vascular Pharmacology Why are People with “Poor Lung Function” At Increased Atherothrombotic Risk?A Critical Review with Potential Therapeutic Indications
Current Vascular Pharmacology The Central Role of Angiotensin I-Converting Enzyme in Vertebrate Pathophysiology
Current Topics in Medicinal Chemistry The Antioxidants and Pro-Antioxidants Network: An Overview
Current Pharmaceutical Design