Abstract
The cannabinoid CB2 receptor continues to be an intriguing target for the potential therapeutic benefit of cannabinoids. Because this receptor is significantly found outside the brain, compounds specific for the CB2 receptor may be free of the side effects that have plagued cannabinoid CB1 receptor-based therapeutics. In this review, we will discuss a class of compounds which modulate the constitutive activity of the cannabinoid CB2 receptor, the inverse agonists. We will discuss recent chemical advances that provide new compounds to investigate the biology based on this pharmacology. We will then discuss new biology associated with the cannabinoid CB2 receptor for hints of how these compounds can best be utilized in vivo.
Keywords: Cannabinoid CB2 receptor, inverse agonist, constitutive activity, inflammation, migration, cannabidiol
Current Topics in Medicinal Chemistry
Title: Updating the Chemistry and Biology of Cannabinoid CB2 Receptor – Specific Inverse Agonists
Volume: 10 Issue: 8
Author(s): Charles A. Lunn
Affiliation:
Keywords: Cannabinoid CB2 receptor, inverse agonist, constitutive activity, inflammation, migration, cannabidiol
Abstract: The cannabinoid CB2 receptor continues to be an intriguing target for the potential therapeutic benefit of cannabinoids. Because this receptor is significantly found outside the brain, compounds specific for the CB2 receptor may be free of the side effects that have plagued cannabinoid CB1 receptor-based therapeutics. In this review, we will discuss a class of compounds which modulate the constitutive activity of the cannabinoid CB2 receptor, the inverse agonists. We will discuss recent chemical advances that provide new compounds to investigate the biology based on this pharmacology. We will then discuss new biology associated with the cannabinoid CB2 receptor for hints of how these compounds can best be utilized in vivo.
Export Options
About this article
Cite this article as:
A. Lunn Charles, Updating the Chemistry and Biology of Cannabinoid CB2 Receptor – Specific Inverse Agonists, Current Topics in Medicinal Chemistry 2010; 10 (8) . https://dx.doi.org/10.2174/156802610791164193
DOI https://dx.doi.org/10.2174/156802610791164193 |
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
-
Palmitoylated Prolactin-releasing Peptide Reduced Aβ Plaques and Microgliosis in the Cerebellum: APP/PS1 Mice Study
Current Alzheimer Research Involvement of Cytosolic Phospholipase A2, Calcium Independent Phospholipase A2 and Plasmalogen Selective Phospholipase A2 in Neurodegenerative and Neuropsychiatric Conditions
Current Medicinal Chemistry The Endothelin Axis as Therapeutic Target in Human Malignancies: Present and Future
Current Pharmaceutical Design Double-Edged Effects of Arsenic Compounds: Anticancer and Carcinogenic Effects
Current Drug Metabolism Cardiovascular Side Effects of New Antidepressants and Antipsychotics: New Drugs, old Concerns?
Current Pharmaceutical Design Viral Induced Oxidative and Inflammatory Response in Alzheimer’s Disease Pathogenesis with Identification of Potential Drug Candidates: A Systematic Review using Systems Biology Approach
Current Neuropharmacology Inhibition of Early Biochemical Defects in Prodromal Huntington’s disease by Simultaneous Activation of Nrf2 and Elevation of Multiple Micronutrients
Current Aging Science Oncolytic Herpes Simplex Virus Type 1 and Host Immune Responses
Current Cancer Drug Targets Ladostigil: A Novel Multimodal Neuroprotective Drug with Cholinesterase and Brain-Selective Monoamine Oxidase Inhibitory Activities for Alzheimers Disease Treatment
Current Drug Targets miRNA-497 Enhances the Sensitivity of Colorectal Cancer Cells to Neoadjuvant Chemotherapeutic Drug
Current Protein & Peptide Science Pharmacologic Evidence of Green Tea in Targeting Tyrosine Kinases
Current Reviews in Clinical and Experimental Pharmacology Cholesterol Homeostasis Failure in the Brain: Implications for Synaptic Dysfunction and Cognitive Decline
Current Medicinal Chemistry Natural Products Targeting Cancer Stem Cells: A Revisit
Current Medicinal Chemistry Neurotrophic Actions of Mood-Stabilizers: A Recent Research Discovery and its Potential Clinical Applications
Current Psychiatry Reviews The Cholesterol Transport Inhibitor U18666a Regulates Amyloid Precursor Protein Metabolism and Trafficking in N2aAPP “Swedish” Cells
Current Alzheimer Research Preparation and Quality Control of <sup>111</sup>In-Plerixafor for Chemokine Receptor CXCR4
Recent Patents and Topics on Imaging (Discontinued) An Effective HIV Vaccine: A Combination of Humoral and Cellular Immunity?
Current HIV Research Na<sup>+</sup>/K<sup>+</sup> ATPase Inhibitors in Cancer
Current Drug Targets Clinical Pharmacology of Cyclophosphamide and Ifosfamide
Current Drug Therapy Incorporation of Anti-angiogenic Therapies in the Treatment of Epithelial Ovarian Cancer: Current Perspectives and Future Directions
Current Angiogenesis (Discontinued)