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Since Rimonabant was withdrawn in Europe in 2008 because of its substantial CNS risk factors including depression and anxiety, the development of anti-obesity drugs targeting CB1R in the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Abstract: Since Rimonabant was withdrawn in Europe in 2008 because of its substantial CNS risk factors including depression and anxiety, the development of anti-obesity drugs targeting CB1R in the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
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
-
Atherogenesis in White Coat Hypertension
Current Hypertension Reviews Inflammation as the Common Biological Link Between Depression and Cardiovascular Diseases: Can Carnosine Exert a Protective Role?
Current Medicinal Chemistry Recent Patents on Stimuli Responsive Hydrogel Drug Delivery System
Recent Patents on Drug Delivery & Formulation Dietary Intake and Physical Activity in a Canadian Population Sample of Male Patients with HIV Infection and Metabolic Abnormalities
Current HIV Research New Pharmacological Approaches to the Prevention of Myocardial Ischemia- Reperfusion Injury
Current Drug Targets Cholesterol Efflux and Reverse Cholesterol Transport: Experimental Approaches
Current Medicinal Chemistry Standardization of QRS Duration Measurement and LBBB Criteria in CRT Trials and Clinical Practice
Current Cardiology Reviews Genetic Polymorphism and Tumor Immunotherapy
Current Pharmacogenomics Semicarbazide-Sensitive Amine Oxidase/Vascular Adhesion Protein 1: Recent Developments Concerning Substrates and Inhibitors of a Promising Therapeutic Target
Current Medicinal Chemistry The Endothelial-Mesenchymal Transition (EndMT) and Tissue Regeneration
Current Stem Cell Research & Therapy Differential Regulation of microRNAs in Patients with Ischemic Stroke
Current Neurovascular Research Production and Purification of Functional Lipids Through Enzymatic and Microorganism-Mediated Processes
Current Organic Chemistry Anti-Inflammatory Therapy in Uveitis
Recent Patents on Inflammation & Allergy Drug Discovery Pharmacological Applications of Antioxidants: Lights and Shadows
Current Drug Targets Efficacy and Cardiovascular Safety of Metformin
Current Drug Safety Sleep Duration as a Risk Factor for Cardiovascular Disease- a Review of the Recent Literature
Current Cardiology Reviews Pluripotent Stem Cell Derivation and Differentiation Toward Cardiac Muscle: Novel Techniques and Advances in Patent Literature
Recent Patents on Drug Delivery & Formulation ECG Analysis: A Brief Review
Recent Advances in Computer Science and Communications Alterations in the Vascular Reactivity of Aorta in the Early and Late Phase of Adjuvant-Induced Arthritis in Rat
Vascular Disease Prevention (Discontinued) Inflammatory Markers Associated With Diabetes Mellitus – Old and New Players
Current Pharmaceutical Design