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Natural Negative Allosteric Modulators of 5-HT(3) Receptors
Chemotherapy-induced nausea and vomiting (CINV) remain the most common and devastating side-effects associated with cancer chemotherapy. In recent decades, several lines of research emphasize the importance of 5-hydroxytryptamine3 (5-HT(3;) serotonin) receptors in the pathogenesis and treatment of C...
Autores principales: | , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2018
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6321066/ https://www.ncbi.nlm.nih.gov/pubmed/30513973 http://dx.doi.org/10.3390/molecules23123186 |
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author | Al Kury, Lina T. Mahgoub, Mohamed Howarth, Frank Christopher Oz, Murat |
author_facet | Al Kury, Lina T. Mahgoub, Mohamed Howarth, Frank Christopher Oz, Murat |
author_sort | Al Kury, Lina T. |
collection | PubMed |
description | Chemotherapy-induced nausea and vomiting (CINV) remain the most common and devastating side-effects associated with cancer chemotherapy. In recent decades, several lines of research emphasize the importance of 5-hydroxytryptamine3 (5-HT(3;) serotonin) receptors in the pathogenesis and treatment of CINV. 5-HT(3) receptors are members of ligand-gated ion channels that mediate the rapid and transient membrane-depolarizing effect of 5-HT in the central and peripheral nervous system. These receptors play important roles in nausea and vomiting, as well as regulation of peristalsis and pain transmission. The development of antagonists for 5-HT(3) receptor dramatically improved the treatment of CINV in cancer patients. In fact, the most common use of 5-HT(3) receptor antagonists to date is the treatment of nausea and vomiting. In recent years, there has been an increasing tendency to use natural plant products as important therapeutic entities in the treatment of various diseases. In this article, we examined the results of earlier studies on the actions of natural compounds on the functional properties of 5-HT(3) receptors. It is likely that these natural modulators of 5-HT(3) receptors can be employed as lead structures for the synthesis of therapeutic agents for treating CINV in future clinical studies. |
format | Online Article Text |
id | pubmed-6321066 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2018 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-63210662019-01-14 Natural Negative Allosteric Modulators of 5-HT(3) Receptors Al Kury, Lina T. Mahgoub, Mohamed Howarth, Frank Christopher Oz, Murat Molecules Review Chemotherapy-induced nausea and vomiting (CINV) remain the most common and devastating side-effects associated with cancer chemotherapy. In recent decades, several lines of research emphasize the importance of 5-hydroxytryptamine3 (5-HT(3;) serotonin) receptors in the pathogenesis and treatment of CINV. 5-HT(3) receptors are members of ligand-gated ion channels that mediate the rapid and transient membrane-depolarizing effect of 5-HT in the central and peripheral nervous system. These receptors play important roles in nausea and vomiting, as well as regulation of peristalsis and pain transmission. The development of antagonists for 5-HT(3) receptor dramatically improved the treatment of CINV in cancer patients. In fact, the most common use of 5-HT(3) receptor antagonists to date is the treatment of nausea and vomiting. In recent years, there has been an increasing tendency to use natural plant products as important therapeutic entities in the treatment of various diseases. In this article, we examined the results of earlier studies on the actions of natural compounds on the functional properties of 5-HT(3) receptors. It is likely that these natural modulators of 5-HT(3) receptors can be employed as lead structures for the synthesis of therapeutic agents for treating CINV in future clinical studies. MDPI 2018-12-03 /pmc/articles/PMC6321066/ /pubmed/30513973 http://dx.doi.org/10.3390/molecules23123186 Text en © 2018 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Review Al Kury, Lina T. Mahgoub, Mohamed Howarth, Frank Christopher Oz, Murat Natural Negative Allosteric Modulators of 5-HT(3) Receptors |
title | Natural Negative Allosteric Modulators of 5-HT(3) Receptors |
title_full | Natural Negative Allosteric Modulators of 5-HT(3) Receptors |
title_fullStr | Natural Negative Allosteric Modulators of 5-HT(3) Receptors |
title_full_unstemmed | Natural Negative Allosteric Modulators of 5-HT(3) Receptors |
title_short | Natural Negative Allosteric Modulators of 5-HT(3) Receptors |
title_sort | natural negative allosteric modulators of 5-ht(3) receptors |
topic | Review |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6321066/ https://www.ncbi.nlm.nih.gov/pubmed/30513973 http://dx.doi.org/10.3390/molecules23123186 |
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