Adenosine receptors as neuroinflammation modulators: role of A1 agonists and A2A antagonists

Detalhes bibliográficos
Autor(a) principal: Martí Navia, Aleix
Data de Publicação: 2020
Outros Autores: Dal Ben, Diego, Lambertucci, Catia, Spinaci, Andrea, Volpini, Rosaria, Marques-Morgado, Inês, Coelho, Joana E, Lopes, Luisa V., Marucci, Gabriella, Buccioni, Michela
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
Texto Completo: http://hdl.handle.net/10451/55387
Resumo: © 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/).
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spelling Adenosine receptors as neuroinflammation modulators: role of A1 agonists and A2A antagonistsA1AR agonistA2AAR antagonistLPSCytokineGliaNeuroinflammation© 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/).The pathological condition of neuroinflammation is caused by the activation of the neuroimmune cells astrocytes and microglia. The autacoid adenosine seems to be an important neuromodulator in this condition. Its main receptors involved in the neuroinflammation modulation are A1AR and A2AAR. Evidence suggests that A1AR activation produces a neuroprotective effect and A2AARs block prevents neuroinflammation. The aim of this work is to elucidate the effects of these receptors in neuroinflammation using the partial agonist 2'-dCCPA (2-chloro-N6-cyclopentyl-2'-deoxyadenosine) (C1 KiA1AR = 550 nM, KiA2AAR = 24,800 nM, and KiA3AR = 5560 nM, α = 0.70, EC50A1AR = 832 nM) and the newly synthesized in house compound 8-chloro-9-ethyl-2-phenethoxyadenine (C2 KiA2AAR = 0.75 nM; KiA1AR = 17 nM and KiA3AR = 227 nM, IC50A2AAR = 251 nM unpublished results). The experiments were performed in in vitro and in in vivo models of neuroinflammation. Results showed that C1 was able to prevent the inflammatory effect induced by cytokine cocktail (TNF-α, IL-1β, and IFN-γ) while C2 possess both anti-inflammatory and antioxidant properties, counteracting both neuroinflammation in mixed glial cells and in an animal model of neuroinflammation. In conclusion, C2 is a potential candidate for neuroinflammation therapy.This research was funded by Cofinanziamento Assegno di Ricerca Volpini-Marucci, n° FPI400037 and by Fundação para a Ciência e a Tecnologia (PTDC/BIM-MEC/47778/2014). This work was supported by the University of Camerino (Fondo di ricerca di Ateneo) and by a grant from the Ministry of Research (PRIN N° 2015E8EMCM_008, 2015).MDPIRepositório da Universidade de LisboaMartí Navia, AleixDal Ben, DiegoLambertucci, CatiaSpinaci, AndreaVolpini, RosariaMarques-Morgado, InêsCoelho, Joana ELopes, Luisa V.Marucci, GabriellaBuccioni, Michela2022-12-14T12:07:09Z20202020-01-01T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleapplication/pdfhttp://hdl.handle.net/10451/55387engCells. 2020 Jul 21;9(7):173910.3390/cells90717392073-4409info:eu-repo/semantics/openAccessreponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãoinstacron:RCAAP2023-11-08T17:02:17Zoai:repositorio.ul.pt:10451/55387Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-19T22:06:02.343676Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãofalse
dc.title.none.fl_str_mv Adenosine receptors as neuroinflammation modulators: role of A1 agonists and A2A antagonists
title Adenosine receptors as neuroinflammation modulators: role of A1 agonists and A2A antagonists
spellingShingle Adenosine receptors as neuroinflammation modulators: role of A1 agonists and A2A antagonists
Martí Navia, Aleix
A1AR agonist
A2AAR antagonist
LPS
Cytokine
Glia
Neuroinflammation
title_short Adenosine receptors as neuroinflammation modulators: role of A1 agonists and A2A antagonists
title_full Adenosine receptors as neuroinflammation modulators: role of A1 agonists and A2A antagonists
title_fullStr Adenosine receptors as neuroinflammation modulators: role of A1 agonists and A2A antagonists
title_full_unstemmed Adenosine receptors as neuroinflammation modulators: role of A1 agonists and A2A antagonists
title_sort Adenosine receptors as neuroinflammation modulators: role of A1 agonists and A2A antagonists
author Martí Navia, Aleix
author_facet Martí Navia, Aleix
Dal Ben, Diego
Lambertucci, Catia
Spinaci, Andrea
Volpini, Rosaria
Marques-Morgado, Inês
Coelho, Joana E
Lopes, Luisa V.
Marucci, Gabriella
Buccioni, Michela
author_role author
author2 Dal Ben, Diego
Lambertucci, Catia
Spinaci, Andrea
Volpini, Rosaria
Marques-Morgado, Inês
Coelho, Joana E
Lopes, Luisa V.
Marucci, Gabriella
Buccioni, Michela
author2_role author
author
author
author
author
author
author
author
author
dc.contributor.none.fl_str_mv Repositório da Universidade de Lisboa
dc.contributor.author.fl_str_mv Martí Navia, Aleix
Dal Ben, Diego
Lambertucci, Catia
Spinaci, Andrea
Volpini, Rosaria
Marques-Morgado, Inês
Coelho, Joana E
Lopes, Luisa V.
Marucci, Gabriella
Buccioni, Michela
dc.subject.por.fl_str_mv A1AR agonist
A2AAR antagonist
LPS
Cytokine
Glia
Neuroinflammation
topic A1AR agonist
A2AAR antagonist
LPS
Cytokine
Glia
Neuroinflammation
description © 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/).
publishDate 2020
dc.date.none.fl_str_mv 2020
2020-01-01T00:00:00Z
2022-12-14T12:07:09Z
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv http://hdl.handle.net/10451/55387
url http://hdl.handle.net/10451/55387
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv Cells. 2020 Jul 21;9(7):1739
10.3390/cells9071739
2073-4409
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv MDPI
publisher.none.fl_str_mv MDPI
dc.source.none.fl_str_mv reponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
instacron:RCAAP
instname_str Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
instacron_str RCAAP
institution RCAAP
reponame_str Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
collection Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
repository.name.fl_str_mv Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
repository.mail.fl_str_mv
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