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
-
Targeting Brain Tumors with Nanomedicines: Overcoming Blood Brain Barrier Challenges
Current Clinical Pharmacology Targeting the Endocannabinod System to Limit Myocardial and Cerebral Ischemic and Reperfusion Injury
Current Pharmaceutical Biotechnology Recent Advances in Targeted Therapy for Glioma
Current Medicinal Chemistry Transition Metal Based Anticancer Drugs
Current Topics in Medicinal Chemistry BCL-2 Family Proteins: The Mitochondrial Apoptotic Key Regulators
Current Cancer Therapy Reviews Connecting Parkinsons Disease and Drug Addiction: Common Players Reveal Unexpected Disease Connections and Novel Therapeutic Approaches
Current Pharmaceutical Design Recent Advances in Antabuse (Disulfiram): The Importance of its Metal-binding Ability to its Anticancer Activity
Current Medicinal Chemistry MMPs in Ovarian Cancer as Therapeutic Targets
Anti-Cancer Agents in Medicinal Chemistry Pharmacodynamics of Radiolabelled Anticancer Drugs for Positron Emission Tomography
Current Pharmaceutical Design The Molecular Pathology of Eye Tumors: A 2019 Update Main Interests for Routine Clinical Practice
Current Molecular Medicine Gliomas: New Perspectives in Diagnosis, Treatment and Prognosis
Current Topics in Medicinal Chemistry Targeting CXCL12/CXCR4 Axis in Tumor Immunotherapy
Current Medicinal Chemistry Heterocyclic Amaryllidaceae Alkaloids: Biosynthesis and Pharmacological Applications
Current Topics in Medicinal Chemistry Lipid-Based Drug Delivery Systems for Cancer Treatment
Current Drug Targets Quantitative Proteomics for Cancer Biomarker Discovery
Combinatorial Chemistry & High Throughput Screening Blocking Ca2+ Entry: A Way to Control Cell Proliferation
Current Medicinal Chemistry Hypericin and its Derivatives Act as Radiosensitizing Agents That Can Inhibit Tumor Initiating Cell Viability
Clinical Cancer Drugs Cytotoxic Effects of Chemotherapeutic Drugs and Heterocyclic Compounds at Application on the Cells of Primary Culture of Neuroepithelium Tumors
Medicinal Chemistry DNA Double Strand Breaks Repair Inhibitors: Relevance as Potential New Anticancer Therapeutics
Current Medicinal Chemistry Characterization of Breast Lesions by Magnetic Resonance Imaging (MRI) and Spectroscopy (MRS)
Current Medical Imaging