Past, present and future of A(2A) adenosine receptor antagonists in the therapy of Parkinson's disease

Several selective antagonists for adenosine A2A receptors (A2AR) are currently under evaluation in clinical trials (phases I to III) to treat Parkinson's disease, and they will probably soon reach the market. The usefulness of these antagonists has been deduced from studies demonstrating functi...

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Detalhes bibliográficos
Autores: Armentero, Marie Therese, Pinna, Annalisa, Ferré, Sergi, Lanciego, José Luis, Müller, Christa E., Franco Fernández, Rafael
Formato: artículo
Estado:Versión aceptada para publicación
Fecha de publicación:2011
País:España
Recursos:Universidad de Barcelona
Repositorio:Dipòsit Digital de la UB
OAI Identifier:oai:diposit.ub.edu:2445/126553
Acesso em linha:https://hdl.handle.net/2445/126553
Access Level:acceso abierto
Palavra-chave:Adenosina
Malaltia de Parkinson
Receptors cel·lulars
Adenosine
Parkinson's disease
Cell receptors
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spelling Past, present and future of A(2A) adenosine receptor antagonists in the therapy of Parkinson's diseaseArmentero, Marie TheresePinna, AnnalisaFerré, SergiLanciego, José LuisMüller, Christa E.Franco Fernández, RafaelAdenosinaMalaltia de ParkinsonReceptors cel·lularsAdenosineParkinson's diseaseCell receptorsSeveral selective antagonists for adenosine A2A receptors (A2AR) are currently under evaluation in clinical trials (phases I to III) to treat Parkinson's disease, and they will probably soon reach the market. The usefulness of these antagonists has been deduced from studies demonstrating functional interactions between dopamine D2 and adenosine A2A receptors in the basal ganglia. At present it is believed that A2AR antagonists can be used in combination with the dopamine precursor L-DOPA to minimize the motor symptoms of Parkinson's patients. However, a considerable body of data indicates that in addition to ameliorating motor symptoms, adenosine A2AR antagonists may also prevent neurodegeneration. Despite these promising indications, one further issue must be considered in order to develop fully optimized antiparkinsonian drug therapy, namely the existence of (hetero)dimers/oligomers of G protein-coupled receptors, a topic that is currently the focus of intense debate within the scientific community. Dopamine D2 receptors (D2Rs) expressed in the striatum are known to form heteromers with A2A adenosine receptors. Thus, the development of heteromer-specific A2A receptor antagonists represents a promising strategy for the identification of more selective and safer drugs.Elsevier2011info:eu-repo/semantics/articleinfo:eu-repo/semantics/acceptedVersionapplication/pdfhttps://hdl.handle.net/2445/126553Articles publicats en revistes (Bioquímica i Biomedicina Molecular)reponame:Dipòsit Digital de la UBinstname:Universidad de BarcelonaInglésVersió postprint del document publicat a: https://doi.org/10.1016/j.pharmthera.2011.07.004Pharmacology & Therapeutics, 2011, vol. 132, num. 3, p. 280-299https://doi.org/10.1016/j.pharmthera.2011.07.004(c) Elsevier, 2011info:eu-repo/semantics/openAccessoai:diposit.ub.edu:2445/1265532026-05-27T06:46:51Z
dc.title.none.fl_str_mv Past, present and future of A(2A) adenosine receptor antagonists in the therapy of Parkinson's disease
title Past, present and future of A(2A) adenosine receptor antagonists in the therapy of Parkinson's disease
spellingShingle Past, present and future of A(2A) adenosine receptor antagonists in the therapy of Parkinson's disease
Armentero, Marie Therese
Adenosina
Malaltia de Parkinson
Receptors cel·lulars
Adenosine
Parkinson's disease
Cell receptors
title_short Past, present and future of A(2A) adenosine receptor antagonists in the therapy of Parkinson's disease
title_full Past, present and future of A(2A) adenosine receptor antagonists in the therapy of Parkinson's disease
title_fullStr Past, present and future of A(2A) adenosine receptor antagonists in the therapy of Parkinson's disease
title_full_unstemmed Past, present and future of A(2A) adenosine receptor antagonists in the therapy of Parkinson's disease
title_sort Past, present and future of A(2A) adenosine receptor antagonists in the therapy of Parkinson's disease
dc.creator.none.fl_str_mv Armentero, Marie Therese
Pinna, Annalisa
Ferré, Sergi
Lanciego, José Luis
Müller, Christa E.
Franco Fernández, Rafael
author Armentero, Marie Therese
author_facet Armentero, Marie Therese
Pinna, Annalisa
Ferré, Sergi
Lanciego, José Luis
Müller, Christa E.
Franco Fernández, Rafael
author_role author
author2 Pinna, Annalisa
Ferré, Sergi
Lanciego, José Luis
Müller, Christa E.
Franco Fernández, Rafael
author2_role author
author
author
author
author
dc.subject.none.fl_str_mv Adenosina
Malaltia de Parkinson
Receptors cel·lulars
Adenosine
Parkinson's disease
Cell receptors
topic Adenosina
Malaltia de Parkinson
Receptors cel·lulars
Adenosine
Parkinson's disease
Cell receptors
description Several selective antagonists for adenosine A2A receptors (A2AR) are currently under evaluation in clinical trials (phases I to III) to treat Parkinson's disease, and they will probably soon reach the market. The usefulness of these antagonists has been deduced from studies demonstrating functional interactions between dopamine D2 and adenosine A2A receptors in the basal ganglia. At present it is believed that A2AR antagonists can be used in combination with the dopamine precursor L-DOPA to minimize the motor symptoms of Parkinson's patients. However, a considerable body of data indicates that in addition to ameliorating motor symptoms, adenosine A2AR antagonists may also prevent neurodegeneration. Despite these promising indications, one further issue must be considered in order to develop fully optimized antiparkinsonian drug therapy, namely the existence of (hetero)dimers/oligomers of G protein-coupled receptors, a topic that is currently the focus of intense debate within the scientific community. Dopamine D2 receptors (D2Rs) expressed in the striatum are known to form heteromers with A2A adenosine receptors. Thus, the development of heteromer-specific A2A receptor antagonists represents a promising strategy for the identification of more selective and safer drugs.
publishDate 2011
dc.date.none.fl_str_mv 2011
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/acceptedVersion
format article
status_str acceptedVersion
dc.identifier.none.fl_str_mv https://hdl.handle.net/2445/126553
url https://hdl.handle.net/2445/126553
dc.language.none.fl_str_mv Inglés
language_invalid_str_mv Inglés
dc.relation.none.fl_str_mv Versió postprint del document publicat a: https://doi.org/10.1016/j.pharmthera.2011.07.004
Pharmacology & Therapeutics, 2011, vol. 132, num. 3, p. 280-299
https://doi.org/10.1016/j.pharmthera.2011.07.004
dc.rights.none.fl_str_mv (c) Elsevier, 2011
info:eu-repo/semantics/openAccess
rights_invalid_str_mv (c) Elsevier, 2011
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv Elsevier
publisher.none.fl_str_mv Elsevier
dc.source.none.fl_str_mv Articles publicats en revistes (Bioquímica i Biomedicina Molecular)
reponame:Dipòsit Digital de la UB
instname:Universidad de Barcelona
instname_str Universidad de Barcelona
reponame_str Dipòsit Digital de la UB
collection Dipòsit Digital de la UB
repository.name.fl_str_mv
repository.mail.fl_str_mv
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score 15.301603

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