Abstract
The 5-HT3 receptor is a member of the Cys-loop family of ligand-gated ion channels. These receptors are located in both the peripheral and central nervous systems, where functional receptors are constructed from five subunits. These subunits may be the same (homopentameric 5-HT3A receptors) or different (heteropentameric receptors, usually comprising of 5-HT3A and 5-HT3B receptor subunits), with the latter having a number of distinct properties. The 5-HT3 receptor binding site is comprised of six loops from two adjacent subunits, and critical ligand binding amino acids in these loops have been largely identified. There are a range of selective agonists and antagonists for these receptors and the pharmacophore is reasonably well understood. There are also a wide range of compounds that can modulate receptor activity. Studies have suggested many diverse potential disease targets that might be amenable to alleviation by 5-HT3 receptor selective compounds but to date only two applications have been fully realised in the clinic: the treatment of emesis and irritable-bowel syndrome.
Keywords: Serotonin receptor, ligand-gated ion channel, 5-HT3 receptor, ligand binding, antagonist, agonist, pharmacology, disease
Current Pharmaceutical Design
Title: 5-HT3 Receptors
Volume: 12 Issue: 28
Author(s): A. J. Thompson and S. C. R. Lummis
Affiliation:
Keywords: Serotonin receptor, ligand-gated ion channel, 5-HT3 receptor, ligand binding, antagonist, agonist, pharmacology, disease
Abstract: The 5-HT3 receptor is a member of the Cys-loop family of ligand-gated ion channels. These receptors are located in both the peripheral and central nervous systems, where functional receptors are constructed from five subunits. These subunits may be the same (homopentameric 5-HT3A receptors) or different (heteropentameric receptors, usually comprising of 5-HT3A and 5-HT3B receptor subunits), with the latter having a number of distinct properties. The 5-HT3 receptor binding site is comprised of six loops from two adjacent subunits, and critical ligand binding amino acids in these loops have been largely identified. There are a range of selective agonists and antagonists for these receptors and the pharmacophore is reasonably well understood. There are also a wide range of compounds that can modulate receptor activity. Studies have suggested many diverse potential disease targets that might be amenable to alleviation by 5-HT3 receptor selective compounds but to date only two applications have been fully realised in the clinic: the treatment of emesis and irritable-bowel syndrome.
Export Options
About this article
Cite this article as:
Thompson J. A. and R. Lummis C. S., 5-HT3 Receptors, Current Pharmaceutical Design 2006; 12 (28) . https://dx.doi.org/10.2174/138161206778522029
DOI https://dx.doi.org/10.2174/138161206778522029 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...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
-
Replicative Oncolytic Herpes Simplex Viruses in Combination Cancer Therapies
Current Gene Therapy Withdrawal Notice: Drug Repurposing for Prospective Anti-Cancer Agents Along with the Clinical Status of the Repurposed Drug
Anti-Cancer Agents in Medicinal Chemistry Microglia in Alzheimer's Disease: The Good, the Bad and the Ugly
Current Alzheimer Research Role of EGFR Inhibitors in the Treatment of Central Nervous System Metastases from Non-Small Cell Lung Cancer
Current Cancer Drug Targets A Validated Mathematical Model of Tumour-Immune Interactions for Glioblastoma
Current Medical Imaging PLGA Hollow Microbubbles Loaded with Iron Oxide Nanoparticles and Doxorubicin for Dual-mode US/MR Imaging and Drug Delivery
Current Nanoscience Aurora A and B Kinases - Targets of Novel Anticancer Drugs
Recent Patents on Anti-Cancer Drug Discovery Chemotherapeutic Targeting of Cell Death Pathways
Anti-Cancer Agents in Medicinal Chemistry Cytotoxic and Anticancer Activities of Isatin and Its Derivatives: A Comprehensive Review from 2000-2008
Anti-Cancer Agents in Medicinal Chemistry Mechanisms of Tubulin Binding Ligands to Target Cancer Cells: Updates on their Therapeutic Potential and Clinical Trials
Current Cancer Drug Targets Natural Antibodies: Protecting Role of IgM in Glioblastoma and Brain Tumours
Current Pharmaceutical Design Radiolabelled Oligonucleotides for Imaging of Gene Expression with PET
Current Medicinal Chemistry Clinical Trials with Oncolytic Adenovirus in China
Current Cancer Drug Targets Antitumor Activity of Copper (I)–Nicotinate Complex and Autophagy Modulation in HCC1806 Breast Cancer Cells
Anti-Cancer Agents in Medicinal Chemistry Brain Delivery Systems via Mechanism Independent of Receptor-Mediated Endocytosis and Adsorptive-Mediated Endocytosis
Current Pharmaceutical Biotechnology Resveratrol and Ischemic Preconditioning in the Brain
Current Medicinal Chemistry Drug Delivery Nanosystems in Glioblastoma Multiforme Treatment: Current State of the Art
Current Neuropharmacology Erythropoietin in Stroke Therapy: Friend or Foe
Current Medicinal Chemistry RNA Splicing: Basic Aspects Underlie Antitumor Targeting
Recent Patents on Anti-Cancer Drug Discovery Radiation and Gene Therapy: Rays of Hope for the New Millennium?
Current Gene Therapy