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Targeting Adenosine Receptors: A Potential Pharmacological Avenue for Acute and Chronic Pain
Adenosine is a purine nucleoside, responsible for the regulation of multiple physiological and pathological cellular and tissue functions by activation of four G protein-coupled receptors (GPCR), namely A(1), A(2A), A(2B), and A(3) adenosine receptors (ARs). In recent years, extensive progress has b...
Autores principales: | , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2020
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7698931/ https://www.ncbi.nlm.nih.gov/pubmed/33218074 http://dx.doi.org/10.3390/ijms21228710 |
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author | Vincenzi, Fabrizio Pasquini, Silvia Borea, Pier Andrea Varani, Katia |
author_facet | Vincenzi, Fabrizio Pasquini, Silvia Borea, Pier Andrea Varani, Katia |
author_sort | Vincenzi, Fabrizio |
collection | PubMed |
description | Adenosine is a purine nucleoside, responsible for the regulation of multiple physiological and pathological cellular and tissue functions by activation of four G protein-coupled receptors (GPCR), namely A(1), A(2A), A(2B), and A(3) adenosine receptors (ARs). In recent years, extensive progress has been made to elucidate the role of adenosine in pain regulation. Most of the antinociceptive effects of adenosine are dependent upon A(1)AR activation located at peripheral, spinal, and supraspinal sites. The role of A(2A)AR and A(2B)AR is more controversial since their activation has both pro- and anti-nociceptive effects. A(3)AR agonists are emerging as promising candidates for neuropathic pain. Although their therapeutic potential has been demonstrated in diverse preclinical studies, no AR ligands have so far reached the market. To date, novel pharmacological approaches such as adenosine regulating agents and allosteric modulators have been proposed to improve efficacy and limit side effects enhancing the effect of endogenous adenosine. This review aims to provide an overview of the therapeutic potential of ligands interacting with ARs and the adenosinergic system for the treatment of acute and chronic pain. |
format | Online Article Text |
id | pubmed-7698931 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-76989312020-11-29 Targeting Adenosine Receptors: A Potential Pharmacological Avenue for Acute and Chronic Pain Vincenzi, Fabrizio Pasquini, Silvia Borea, Pier Andrea Varani, Katia Int J Mol Sci Review Adenosine is a purine nucleoside, responsible for the regulation of multiple physiological and pathological cellular and tissue functions by activation of four G protein-coupled receptors (GPCR), namely A(1), A(2A), A(2B), and A(3) adenosine receptors (ARs). In recent years, extensive progress has been made to elucidate the role of adenosine in pain regulation. Most of the antinociceptive effects of adenosine are dependent upon A(1)AR activation located at peripheral, spinal, and supraspinal sites. The role of A(2A)AR and A(2B)AR is more controversial since their activation has both pro- and anti-nociceptive effects. A(3)AR agonists are emerging as promising candidates for neuropathic pain. Although their therapeutic potential has been demonstrated in diverse preclinical studies, no AR ligands have so far reached the market. To date, novel pharmacological approaches such as adenosine regulating agents and allosteric modulators have been proposed to improve efficacy and limit side effects enhancing the effect of endogenous adenosine. This review aims to provide an overview of the therapeutic potential of ligands interacting with ARs and the adenosinergic system for the treatment of acute and chronic pain. MDPI 2020-11-18 /pmc/articles/PMC7698931/ /pubmed/33218074 http://dx.doi.org/10.3390/ijms21228710 Text en © 2020 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 Vincenzi, Fabrizio Pasquini, Silvia Borea, Pier Andrea Varani, Katia Targeting Adenosine Receptors: A Potential Pharmacological Avenue for Acute and Chronic Pain |
title | Targeting Adenosine Receptors: A Potential Pharmacological Avenue for Acute and Chronic Pain |
title_full | Targeting Adenosine Receptors: A Potential Pharmacological Avenue for Acute and Chronic Pain |
title_fullStr | Targeting Adenosine Receptors: A Potential Pharmacological Avenue for Acute and Chronic Pain |
title_full_unstemmed | Targeting Adenosine Receptors: A Potential Pharmacological Avenue for Acute and Chronic Pain |
title_short | Targeting Adenosine Receptors: A Potential Pharmacological Avenue for Acute and Chronic Pain |
title_sort | targeting adenosine receptors: a potential pharmacological avenue for acute and chronic pain |
topic | Review |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7698931/ https://www.ncbi.nlm.nih.gov/pubmed/33218074 http://dx.doi.org/10.3390/ijms21228710 |
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