Abstract
Cannabinoid receptors, belonging to the superfamily of G-protein coupled receptors, play a major role in pathophysiology of a wide range of disparate diseases. Cannabinoid CB2 receptor, which mainly locates in peripheral tissues, represents as a promising drug target for the treatment of pain, osteoporosis, liver disorders, and so on without serious CNS side effects. In the past decades, the identification and optimization of selective ligands for the CB2 receptor has been a major objective in drug discovery. In the present review, we describe recent advances in the development of novel chemotypes of the CB2 receptor selective ligands, and give a simple discussion for the corresponding structureactivity relationships of them.
Keywords: Cannabinoid receptors, CB2, GPCRs, selective ligand, structure-activity relationship.
Mini-Reviews in Medicinal Chemistry
Title:Latest Progress in the Identification of Novel Synthetic Ligands for the Cannabinoid CB2 Receptor
Volume: 14 Issue: 5
Author(s): Shuang Han, Jiong-Jiong Chen and Jian-Zhong Chen
Affiliation:
Keywords: Cannabinoid receptors, CB2, GPCRs, selective ligand, structure-activity relationship.
Abstract: Cannabinoid receptors, belonging to the superfamily of G-protein coupled receptors, play a major role in pathophysiology of a wide range of disparate diseases. Cannabinoid CB2 receptor, which mainly locates in peripheral tissues, represents as a promising drug target for the treatment of pain, osteoporosis, liver disorders, and so on without serious CNS side effects. In the past decades, the identification and optimization of selective ligands for the CB2 receptor has been a major objective in drug discovery. In the present review, we describe recent advances in the development of novel chemotypes of the CB2 receptor selective ligands, and give a simple discussion for the corresponding structureactivity relationships of them.
Export Options
About this article
Cite this article as:
Han Shuang, Chen Jiong-Jiong and Chen Jian-Zhong, Latest Progress in the Identification of Novel Synthetic Ligands for the Cannabinoid CB2 Receptor, Mini-Reviews in Medicinal Chemistry 2014; 14 (5) . https://dx.doi.org/10.2174/1389557514666140428105753
DOI https://dx.doi.org/10.2174/1389557514666140428105753 |
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
-
MicroRNA Expression Analysis of Adult-Onset Drosophila Alzheimer`s Disease Model
Current Alzheimer Research Evidence that Ingested Aluminum Additives Contained in Processed Foods and Alum-Treated Drinking Water are a Major Risk Factor for Alzheimers Disease
Current Inorganic Chemistry (Discontinued) Microenvironmental Determinants of Adult Neural Stem Cell Proliferation and Lineage Commitment in the Healthy and Injured Central Nervous System
Current Stem Cell Research & Therapy Calcium-Sensing Receptors of Human Astrocyte-Neuron Teams: Amyloid-β-Driven Mediators and Therapeutic Targets of Alzheimer's Disease
Current Neuropharmacology Serum Fragments of Tau for the Differential Diagnosis of Alzheimer's Disease
Current Alzheimer Research Therapeutic Potential and Mechanisms of Action of Mesenchymal Stromal Cells for Acute Respiratory Distress Syndrome
Current Stem Cell Research & Therapy Identification of Potent Caspase-3 Inhibitors for Treatment of Multi- Neurodegenerative Diseases Using Pharmacophore Modeling and Docking Approaches
CNS & Neurological Disorders - Drug Targets Mechanisms of Acupuncture Effect on Alzheimer’s Disease in Animal- Based Researches
Current Topics in Medicinal Chemistry Role and Therapeutic Potential of Astrocytes in Amyotrophic Lateral Sclerosis
Current Pharmaceutical Design Aβ1-40 and Aβ1-42 Plasmatic Levels In Stroke: Influence of Pre-Existing Cognitive Status and Stroke Characteristics#
Current Alzheimer Research Calpain-1 and Calpain-2 in the Brain: Dr. Jekill and Mr Hyde?
Current Neuropharmacology Synthesis, Crystal Structure, Anti-inflammatory and Anti-hyperglycemic Activities of Novel 3,4-Disubstituted 1,2,4-Triazol-5(4H)-one Derivatives
Medicinal Chemistry Emerging Perspectives on DNA Double-strand Breaks in Neurodegenerative Diseases
Current Neuropharmacology Implication of Oncogenic Signaling Pathways as a Treatment Strategy for Neurodegenerative Disorders – Contemporary Approaches
CNS & Neurological Disorders - Drug Targets Applications of Indan-1,3-Dione in Heterocyclic Synthesis
Current Organic Synthesis Potential Benefits and Limits of Psychopharmacological Therapies in Pervasive Developmental Disorders
Current Clinical Pharmacology Interaction of Different Proteins with GABA<sub>A</sub> Receptor and their Modulatory Effect on Inhibitory Neural Transmission Leads to Epilepsy
CNS & Neurological Disorders - Drug Targets Is Human Immunodeficiency Virus-Mediated Dementia an Autophagic Defect that Leads to Neurodegeneration?
CNS & Neurological Disorders - Drug Targets Nasal Neuro EPO Could be a Reliable Choice for Neuroprotective Stroke Treatment
Central Nervous System Agents in Medicinal Chemistry The Effects of Variants in the Parkin, PINK1, and DJ-1 Genes along with Evidence for their Pathogenicity
Current Protein & Peptide Science