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
-
Targeted Taxane Delivery Systems: Recent Advances
Drug Delivery Letters L-Thyroxine Acts as a Hormone as well as a Prohormone at the Cell Membrane
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) The Implications of Sortilin/Vps10p Domain Receptors in Neurological and Human Diseases
CNS & Neurological Disorders - Drug Targets Breast Cancer Resistance Protein: A Potential Therapeutic Target for Cancer
Current Drug Targets Inhibition of Apoptosis in Pediatric Cancer by Survivin
Current Pediatric Reviews Delivery and Application of Dietary Polyphenols to Target Organs, Tissues and Intracellular Organelles
Current Drug Metabolism Dual Inhibitors of PI3K/mTOR or mTOR-Selective Inhibitors: Which Way Shall We Go?
Current Medicinal Chemistry Analysis of miRNAs Targeting 3’UTR of H2AFX Gene: a General <i>in Silico</i> Approach
MicroRNA Targeting βIII-Tubulin in Glioblastoma Multiforme: From Cell Biology and Histopathology to Cancer Therapeutics
Anti-Cancer Agents in Medicinal Chemistry Radiochemical Evaluation and <i>In Vitro</i> Assessment of the Targeting Ability of a Novel <sup>99m</sup>Tc-HYNIC-RGD for U87MG Human Brain Cancer Cells
Current Radiopharmaceuticals Prognostic Role of Hedgehog-GLI1 Signaling Pathway in Aggressive and Metastatic Breast Cancers
Current Drug Metabolism Fluorescence-Guided Malignant Glioma Resections
Current Drug Discovery Technologies Meet the Editorial Board
Current Bioinformatics Fabrication of Poly Hydroxybutyrate-Polyethylene Glycol-Folic Acid Nanoparticles Loaded by Paclitaxel
Current Drug Delivery Blockade of Insulin-Like Growth Factor Type-1 Receptor with Cixutumumab (IMC-A12): A Novel Approach to Treatment for Multiple Cancers
Current Drug Targets Relevance of the Deletion Polymorphisms of the Glutathione S-Transferases GSTT1 and GSTM1 in Pharmacology and Toxicology
Current Drug Metabolism Chidamide Inhibits Cell Proliferation via the PI3K/AKT Pathway in K562 Cells Based on Network Pharmacology and Experimental Validation
Current Pharmaceutical Design Targeting Apoptosis Pathways in Cancer Therapy
Current Cancer Drug Targets Lipid-Based Nanocarriers for CNS-Targeted Drug Delivery
Recent Patents on CNS Drug Discovery (Discontinued) In Vivo Anticancer Activity, Toxicology and Histopathological Studies of the Thiolate Gold(I) Complex [Au(Spyrimidine)(PTA-CH<sub>2</sub>Ph)]Br
Anti-Cancer Agents in Medicinal Chemistry