Abstract
The 5-HT3 receptor (5-HT3R) occupies a special place among the serotonin receptor subtypes because it has been shown to be a ligand-gated ion channel, which is involved in a number of physiological functions and important pathologies. 5-HT3R antagonists have shown an outstanding efficacy in the control of the emesis induced by anticancer chemotherapy and few adverse side-effects, so as to revolutionize the treatment of nausea in cancer patients. This review covers the authors work performed during the past decade in the development of 5-HT3R ligands belonging to the class of arylpiperazine derivatives related to quipazine (quipazine-like arylpiperazines, QLAs) and represents the extension of the review previously published in Current Topics in Medicinal Chemistry in 2002. The discussion is mainly focused on the most significant structure-affinity relationships emerged in the progress of the work and shows how the original ideas have evolved in the recent years.
Current Topics in Medicinal Chemistry
Title: The Interactions of the 5-HT3 Receptor with Quipazine-Like Arylpiperazine Ligands. The Journey Track at the End of the First Decade of the Third Millennium
Volume: 10 Issue: 5
Author(s): Andrea Cappelli, Stefania Butini, Antonella Brizzi, Sandra Gemma, Salvatore Valenti, Germano Giuliani, Maurizio Anzini, Laura Mennuni, Giuseppe Campiani, Vittorio Brizzi and Salvatore Vomero
Affiliation:
Abstract: The 5-HT3 receptor (5-HT3R) occupies a special place among the serotonin receptor subtypes because it has been shown to be a ligand-gated ion channel, which is involved in a number of physiological functions and important pathologies. 5-HT3R antagonists have shown an outstanding efficacy in the control of the emesis induced by anticancer chemotherapy and few adverse side-effects, so as to revolutionize the treatment of nausea in cancer patients. This review covers the authors work performed during the past decade in the development of 5-HT3R ligands belonging to the class of arylpiperazine derivatives related to quipazine (quipazine-like arylpiperazines, QLAs) and represents the extension of the review previously published in Current Topics in Medicinal Chemistry in 2002. The discussion is mainly focused on the most significant structure-affinity relationships emerged in the progress of the work and shows how the original ideas have evolved in the recent years.
Export Options
About this article
Cite this article as:
Cappelli Andrea, Butini Stefania, Brizzi Antonella, Gemma Sandra, Valenti Salvatore, Giuliani Germano, Anzini Maurizio, Mennuni Laura, Campiani Giuseppe, Brizzi Vittorio and Vomero Salvatore, The Interactions of the 5-HT3 Receptor with Quipazine-Like Arylpiperazine Ligands. The Journey Track at the End of the First Decade of the Third Millennium, Current Topics in Medicinal Chemistry 2010; 10 (5) . https://dx.doi.org/10.2174/156802610791111560
DOI https://dx.doi.org/10.2174/156802610791111560 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
AlphaFold in Medicinal Chemistry: Opportunities and Challenges
AlphaFold, a groundbreaking AI tool for protein structure prediction, is revolutionizing drug discovery. Its near-atomic accuracy unlocks new avenues for designing targeted drugs and performing efficient virtual screening. However, AlphaFold's static predictions lack the dynamic nature of proteins, crucial for understanding drug action. This is especially true for multi-domain proteins, ...read more
Artificial intelligence for Natural Products Discovery and Development
Our approach involves using computational methods to predict the potential therapeutic benefits of natural products by considering factors such as drug structure, targets, and interactions. We also employ multitarget analysis to understand the role of drug targets in disease pathways. We advocate for the use of artificial intelligence in predicting ...read more
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
- 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
-
CDK Inhibitors: From the Bench to Clinical Trials
Current Drug Targets Hypoxia-Inducible Factor-1 as Regulator of Angiogenesis in Rheumatoid Arthritis - Therapeutic Implications
Current Medicinal Chemistry Understanding Molecular Pathways and Targets of Brachyury in Epithelial-mesenchymal Transition (EMT) in Human Cancers
Current Cancer Drug Targets How do Glial Cells Contribute to Motor Control?
Current Pharmaceutical Design The Dual Role of Nitric Oxide in Glioma
Current Pharmaceutical Design Extracellular ATP and Neurodegeneration
Current Drug Targets - CNS & Neurological Disorders Understanding Autophagy in Cell Death Control
Current Pharmaceutical Design Anti-Cancer Effects of Citalopram on Hepatocellular Carcinoma Cells Occur via Cytochrome C Release and the Activation of NF-kB
Anti-Cancer Agents in Medicinal Chemistry Endocannabinoid Signaling in Midbrain Dopamine Neurons: More than Physiology?
Current Neuropharmacology Meet Our Editorial Board Member
CNS & Neurological Disorders - Drug Targets Imaging Methods in Gene Therapy of Cancer
Current Gene Therapy The Emerging Role of EMT-related lncRNAs in Therapy Resistance and their Applications as Biomarkers
Current Medicinal Chemistry Nanoparticles in Melanoma
Current Medicinal Chemistry Recent Developments in the Formulation of Nanoliposomal Delivery Systems
Current Nanomaterials Editorial [Hot Topic: Novel Kinase Inhibitors in Cancer Therapy (Guest Editors: Ezra E.W. Cohen and Nikolai G. Rainov)]
Reviews on Recent Clinical Trials Therapeutic Use of Chemokines
Current Pharmaceutical Design Recent Patents Reveal Microtubules as Persistent Promising Target for Novel Drug Development for Cancers
Recent Patents on Anti-Infective Drug Discovery Implications of Nanoscale Based Drug Delivery Systems in Delivery and Targeting Tubulin Binding Agent, Noscapine in Cancer Cells
Current Drug Metabolism PI-3 Kinase-PTEN Signaling Node: An Intercept Point for the Control of Angiogenesis
Current Pharmaceutical Design Small-Molecule Inhibitors of Bcl-2 Family Proteins as Therapeutic Agents in Cancer
Recent Patents on Anti-Cancer Drug Discovery