Abstract
During the last decade there has been a growing interest towards the modulation of the cannabinoid CB1 receptor. The identification of CB1 cannabinoid receptor antagonists has been one of the major advances in cannabinoid research. Thus, the development of these ligands has opened new therapeutic applications. Since the discovery of the first cannabinoid receptor antagonist, rimonabant, by Sanofi in 1994, a large number of structural variations within this chemical series of 1,5-diarylpyrazoles have been described. So far, all attempts to identify novel structures for CB1 antagonists have been based on one or more pharmacophoric elements of the rimonabant structure. The advanced clinical trials of rimonabant confirm the therapeutic potential value of CB1 antagonists for the treatment of obesity. In addition, the results of pharmacological and clinical studies reveal other effective pharmacotherapeutic applications. The current review will mainly focus on the structure-activity relationships that have been established for antagonists/inverse agonists that bind to the CB1 cannabinoid receptors and on their therapeutic applications.
Keywords: Cannabinoid, antagonist, CB1, rimonabant, endocannabinoid
Current Topics in Medicinal Chemistry
Title: CB1 Cannabinoid Antagonists: Structure-Activity Relationships and Potential Therapeutic Applications
Volume: 8 Issue: 3
Author(s): Nadine Jagerovic, Cristina Fernandez-Fernandez and Pilar Goya
Affiliation:
Keywords: Cannabinoid, antagonist, CB1, rimonabant, endocannabinoid
Abstract: During the last decade there has been a growing interest towards the modulation of the cannabinoid CB1 receptor. The identification of CB1 cannabinoid receptor antagonists has been one of the major advances in cannabinoid research. Thus, the development of these ligands has opened new therapeutic applications. Since the discovery of the first cannabinoid receptor antagonist, rimonabant, by Sanofi in 1994, a large number of structural variations within this chemical series of 1,5-diarylpyrazoles have been described. So far, all attempts to identify novel structures for CB1 antagonists have been based on one or more pharmacophoric elements of the rimonabant structure. The advanced clinical trials of rimonabant confirm the therapeutic potential value of CB1 antagonists for the treatment of obesity. In addition, the results of pharmacological and clinical studies reveal other effective pharmacotherapeutic applications. The current review will mainly focus on the structure-activity relationships that have been established for antagonists/inverse agonists that bind to the CB1 cannabinoid receptors and on their therapeutic applications.
Export Options
About this article
Cite this article as:
Jagerovic Nadine, Fernandez-Fernandez Cristina and Goya Pilar, CB1 Cannabinoid Antagonists: Structure-Activity Relationships and Potential Therapeutic Applications, Current Topics in Medicinal Chemistry 2008; 8 (3) . https://dx.doi.org/10.2174/156802608783498050
DOI https://dx.doi.org/10.2174/156802608783498050 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
- 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
-
Prolyl Oligopeptidase: A Rising Star on the Stage of Neuroinflammation Research
CNS & Neurological Disorders - Drug Targets Animal Models for the Development of New Neuropharmacological Therapeutics in the Status Epilepticus
Current Neuropharmacology Adrenomedullin in Cardiovascular Disease: A Useful Biomarker, its Pathological Roles and Therapeutic Application
Current Protein & Peptide Science Roles of Renal Proximal Tubule Transport in the Pathogenesis of Hypertension
Current Hypertension Reviews CPR Technique for Infants and Children
Current Pediatric Reviews Closed-loop Neuropharmacology for Epilepsy: Distant Dream or Future Reality?
Current Neuropharmacology Amyloid A Amyloidosis Secondary to Rheumatoid Arthritis: An Uncommon Yet Important Complication
Current Rheumatology Reviews Potential Mechanisms of Failure in the Sudden Infant Death Syndrome
Current Pediatric Reviews A Review of Voltammetric Methods for Determination of Dopamine Agonists
Current Analytical Chemistry Renal Function Impairment in Patients Undergoing Elective EVAR vs. Elective Open Repair During Follow up Period: A Systematic Review of the Literature
Current Vascular Pharmacology Preparation and Evaluation of Chitosan Submicroparticles Containing Pilocarpine for Glaucoma Therapy
Current Drug Delivery Backbone-Cyclized Peptides: A Critical Review
Current Topics in Medicinal Chemistry Diagnosis, Treatment, and New Developments in Preeclampsia
Current Women`s Health Reviews The Concept of Titration can be Transposed to Fluid Management. But does is Change the Volumes? Randomised Trial on Pleth Variability Index During Fast-Track Colonic Surgery
Current Clinical Pharmacology Pharmacokinetic Drug-drug Interaction of Antibiotics Used in Sepsis Care in China
Current Drug Metabolism Novel Immunotherapies for Hematological Malignancies
Current Molecular Pharmacology Caring for HIV-Infected Patients in the ICU in The Highly Active Antiretroviral Therapy Era
Current HIV Research Current Opinions and Perspectives on the Role of Immune System in the Pathogenesis of Parkinson's Disease
Current Pharmaceutical Design Non-Analgesic Effects of Opioids: Opioid-induced Nausea and Vomiting: Mechanisms and Strategies for their Limitation
Current Pharmaceutical Design Pulmonary Hypertension and Lung Transplantation
Current Hypertension Reviews