Abstract
The discovery of the endocannabinoid system has lead to great strides in research development. At present, two cannabinoid receptors, CB1R and CB2R, are known. They belong to Class A rhodopsin-like GPCRs, and possess a different tissue distribution. Many synthetic compounds have been synthesized and tested for their cannabinoid activity. A particular class among them, the aminoalkylindole derivatives (typified by WIN55212-2) are hypothesized to interact in a binding site different from the main cannabinoid agonists. In this review we report the main aminoalkylindole derivatives, and other compounds which are hypothesized to interact in the same binding site. Furthermore we analyze the pharmacological profiles, the mutagenesis data and the computational models that describe their interaction in the cannabinoid receptors, evaluating the most important aspects for their activity and selectivity.
Keywords: Cannabinoid receptors, CB1R, CB2R, aminoalkylindoles, WIN55212-2
Mini-Reviews in Medicinal Chemistry
Title: Indoles and Related Compounds as Cannabinoid Ligands
Volume: 8 Issue: 4
Author(s): Clementina Manera, Tiziano Tuccinardi and Adriano Martinelli
Affiliation:
Keywords: Cannabinoid receptors, CB1R, CB2R, aminoalkylindoles, WIN55212-2
Abstract: The discovery of the endocannabinoid system has lead to great strides in research development. At present, two cannabinoid receptors, CB1R and CB2R, are known. They belong to Class A rhodopsin-like GPCRs, and possess a different tissue distribution. Many synthetic compounds have been synthesized and tested for their cannabinoid activity. A particular class among them, the aminoalkylindole derivatives (typified by WIN55212-2) are hypothesized to interact in a binding site different from the main cannabinoid agonists. In this review we report the main aminoalkylindole derivatives, and other compounds which are hypothesized to interact in the same binding site. Furthermore we analyze the pharmacological profiles, the mutagenesis data and the computational models that describe their interaction in the cannabinoid receptors, evaluating the most important aspects for their activity and selectivity.
Export Options
About this article
Cite this article as:
Manera Clementina, Tuccinardi Tiziano and Martinelli Adriano, Indoles and Related Compounds as Cannabinoid Ligands, Mini-Reviews in Medicinal Chemistry 2008; 8 (4) . https://dx.doi.org/10.2174/138955708783955935
DOI https://dx.doi.org/10.2174/138955708783955935 |
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
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
Natural Products in Drug Discovery
Natural products have always been one of the important ways of drug discovery due to their novel skeleton and diverse functional group characteristics. According to statistics, between 1981 and 2019, the FDA approved a total of 1,394 small molecule drugs for marketing, of which 930 marketed drugs originated from the ...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
-
Targeting the Cancer-Stroma Interaction: A Potential Approach for Pancreatic Cancer Treatment
Current Pharmaceutical Design miRNAs in Cancer Prevention and Treatment and as Molecular Targets for Natural Product Anticancer Agents
Current Cancer Drug Targets PEDF as an Emerging Therapeutic Candidate for Osteosarcoma
Current Cancer Drug Targets Senescence and Cell Death Pathways and Their Role in Cancer Therapeutic Outcome
Current Medicinal Chemistry Cucurbitacin E, An Experimental Lead Triterpenoid with Anticancer, Immunomodulatory and Novel Effects Against Degenerative Diseases. A Mini-Review
Current Topics in Medicinal Chemistry Nutritional Attributes and Health Application of Seabuckthorn (<i>Hippophae rhamnoides</i> L.) – A Review
Current Nutrition & Food Science Oncolytic Viruses: The Best is Yet to Come
Current Cancer Drug Targets Biomarkers for Systemic Therapy in Ovarian Cancer
Current Cancer Drug Targets Neuroprotective Effects of Citrus Fruit-Derived Flavonoids, Nobiletin and Tangeretin in Alzheimer's and Parkinson's Disease
CNS & Neurological Disorders - Drug Targets Potential Role of Natural Compounds as Anti-Angiogenic Agents in Cancer
Current Vascular Pharmacology Clinical Studies with Targeted Toxins in Malignant Glioma
Reviews on Recent Clinical Trials Challenges in the Design of Clinically Useful Brain-targeted Drug Nanocarriers
Current Medicinal Chemistry Signal Transduction Pathways of Taxanes-Induced Apoptosis
Current Medicinal Chemistry - Anti-Cancer Agents Mechlorethamine based Drug Structures for Intervention of Central Nervous System Tumors
Central Nervous System Agents in Medicinal Chemistry Transition Metal-mediated Uncaging Chemistry in Prodrug Design
Current Topics in Medicinal Chemistry Overcoming the Hurdles of Tumor Immunity by Targeting Regulatory Pathways in Innate and Adaptive Immune Cells
Current Pharmaceutical Design Anti-Cancer Activity of Nitrones and Observations on Mechanism of Action
Anti-Cancer Agents in Medicinal Chemistry In vivo Near-infrared Fluorescence Tumor Imaging Using DiR-loaded Nanocarriers
Current Drug Delivery Delineation of Current Development of Antimitotic Compounds Targeting Cytoskeletal Protein Tubulin and Microtubule in the Cancer Therapy
Current Chemical Biology Metal Based Frameworks for Drug Delivery Systems
Current Topics in Medicinal Chemistry