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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...

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Autores principales: Vincenzi, Fabrizio, Pasquini, Silvia, Borea, Pier Andrea, Varani, Katia
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
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.
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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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