Two new adenosine receptor antagonists for the treatment of Parkinson's disease: istradefylline versus tozadenant

Autores
Perez Lloret, Santiago; Merello, Marcelo Jorge
Año de publicación
2014
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
INTRODUCTION: Adenosine A2A receptors are localized in the brain, mainly within the caudate and putamen nuclei of the basal ganglia. Their activation leads to stimulation of the 'indirect' pathway. Conversely, administration of A2A receptor antagonists leads to inhibition of this pathway, which was translated into reduced hypomotility in several animal models of parkinsonism. AREAS COVERED: In this review, the effects of two A2A receptor antagonists, istradefylline and tozadenant, on parkinsonian symptoms in animal and humans will be discussed. EXPERT OPINION: Animal studies have shown potent antiparkinsonian effects for several A2A receptor antagonists, including istradefylline. In clinical trials, istradefylline reduced OFF time when administered with levodopa, but results are inconclusive. Results with tozadenant are scarce. Modification of thalamic blood flow compatible with reduced inhibition was noted in one small trial, followed by a significant reduction in OFF time in a larger one. Therefore, both drugs show promising efficacy for the reduction of OFF time in levodopa-treated Parkinson's disease patients, but further research is needed in order to obtain definitive conclusions.
Fil: Perez Lloret, Santiago. Fundación para la Lucha contra las Enfermedades Neurológicas de la Infancia. Instituto de Investigaciones Neurológicas "Raúl Carrea"; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Merello, Marcelo Jorge. Fundación para la Lucha contra las Enfermedades Neurológicas de la Infancia. Instituto de Investigaciones Neurológicas "Raúl Carrea"; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Materia
A2a Receptor Antagonists
Adenosine
Motor Fluctuations
Wearing-Off
Nivel de accesibilidad
acceso abierto
Condiciones de uso
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
Repositorio
CONICET Digital (CONICET)
Institución
Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador
oai:ri.conicet.gov.ar:11336/16826
Acceder
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network_acronym_str CONICETDig
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network_name_str CONICET Digital (CONICET)
spelling Two new adenosine receptor antagonists for the treatment of Parkinson's disease: istradefylline versus tozadenantPerez Lloret, SantiagoMerello, Marcelo JorgeA2a Receptor AntagonistsAdenosineMotor FluctuationsWearing-Offhttps://purl.org/becyt/ford/3.1https://purl.org/becyt/ford/3INTRODUCTION: Adenosine A2A receptors are localized in the brain, mainly within the caudate and putamen nuclei of the basal ganglia. Their activation leads to stimulation of the 'indirect' pathway. Conversely, administration of A2A receptor antagonists leads to inhibition of this pathway, which was translated into reduced hypomotility in several animal models of parkinsonism. AREAS COVERED: In this review, the effects of two A2A receptor antagonists, istradefylline and tozadenant, on parkinsonian symptoms in animal and humans will be discussed. EXPERT OPINION: Animal studies have shown potent antiparkinsonian effects for several A2A receptor antagonists, including istradefylline. In clinical trials, istradefylline reduced OFF time when administered with levodopa, but results are inconclusive. Results with tozadenant are scarce. Modification of thalamic blood flow compatible with reduced inhibition was noted in one small trial, followed by a significant reduction in OFF time in a larger one. Therefore, both drugs show promising efficacy for the reduction of OFF time in levodopa-treated Parkinson's disease patients, but further research is needed in order to obtain definitive conclusions.Fil: Perez Lloret, Santiago. Fundación para la Lucha contra las Enfermedades Neurológicas de la Infancia. Instituto de Investigaciones Neurológicas "Raúl Carrea"; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Merello, Marcelo Jorge. Fundación para la Lucha contra las Enfermedades Neurológicas de la Infancia. Instituto de Investigaciones Neurológicas "Raúl Carrea"; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaTaylor & Francis2014-03info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/16826Perez Lloret, Santiago; Merello, Marcelo Jorge; Two new adenosine receptor antagonists for the treatment of Parkinson's disease: istradefylline versus tozadenant; Taylor & Francis; Expert Opinion On Pharmacotherapy; 15; 8; 3-2014; 1097-11071465-65661744-7666enginfo:eu-repo/semantics/altIdentifier/url/http://www.tandfonline.com/doi/abs/10.1517/14656566.2014.903924?journalCode=ieop20info:eu-repo/semantics/altIdentifier/doi/10.1517/14656566.2014.903924info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2026-05-06T16:28:03Zoai:ri.conicet.gov.ar:11336/16826instacron:CONICETInstitucionalhttp://ri.conicet.gov.ar/Organismo científico-tecnológicoNo correspondehttp://ri.conicet.gov.ar/oai/requestdasensio@conicet.gov.ar; lcarlino@conicet.gov.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:34982026-05-06 16:28:03.944CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Two new adenosine receptor antagonists for the treatment of Parkinson's disease: istradefylline versus tozadenant
title Two new adenosine receptor antagonists for the treatment of Parkinson's disease: istradefylline versus tozadenant
spellingShingle Two new adenosine receptor antagonists for the treatment of Parkinson's disease: istradefylline versus tozadenant
Perez Lloret, Santiago
A2a Receptor Antagonists
Adenosine
Motor Fluctuations
Wearing-Off
title_short Two new adenosine receptor antagonists for the treatment of Parkinson's disease: istradefylline versus tozadenant
title_full Two new adenosine receptor antagonists for the treatment of Parkinson's disease: istradefylline versus tozadenant
title_fullStr Two new adenosine receptor antagonists for the treatment of Parkinson's disease: istradefylline versus tozadenant
title_full_unstemmed Two new adenosine receptor antagonists for the treatment of Parkinson's disease: istradefylline versus tozadenant
title_sort Two new adenosine receptor antagonists for the treatment of Parkinson's disease: istradefylline versus tozadenant
dc.creator.none.fl_str_mv Perez Lloret, Santiago
Merello, Marcelo Jorge
author Perez Lloret, Santiago
author_facet Perez Lloret, Santiago
Merello, Marcelo Jorge
author_role author
author2 Merello, Marcelo Jorge
author2_role author
dc.subject.none.fl_str_mv A2a Receptor Antagonists
Adenosine
Motor Fluctuations
Wearing-Off
topic A2a Receptor Antagonists
Adenosine
Motor Fluctuations
Wearing-Off
purl_subject.fl_str_mv https://purl.org/becyt/ford/3.1
https://purl.org/becyt/ford/3
dc.description.none.fl_txt_mv INTRODUCTION: Adenosine A2A receptors are localized in the brain, mainly within the caudate and putamen nuclei of the basal ganglia. Their activation leads to stimulation of the 'indirect' pathway. Conversely, administration of A2A receptor antagonists leads to inhibition of this pathway, which was translated into reduced hypomotility in several animal models of parkinsonism. AREAS COVERED: In this review, the effects of two A2A receptor antagonists, istradefylline and tozadenant, on parkinsonian symptoms in animal and humans will be discussed. EXPERT OPINION: Animal studies have shown potent antiparkinsonian effects for several A2A receptor antagonists, including istradefylline. In clinical trials, istradefylline reduced OFF time when administered with levodopa, but results are inconclusive. Results with tozadenant are scarce. Modification of thalamic blood flow compatible with reduced inhibition was noted in one small trial, followed by a significant reduction in OFF time in a larger one. Therefore, both drugs show promising efficacy for the reduction of OFF time in levodopa-treated Parkinson's disease patients, but further research is needed in order to obtain definitive conclusions.
Fil: Perez Lloret, Santiago. Fundación para la Lucha contra las Enfermedades Neurológicas de la Infancia. Instituto de Investigaciones Neurológicas "Raúl Carrea"; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Merello, Marcelo Jorge. Fundación para la Lucha contra las Enfermedades Neurológicas de la Infancia. Instituto de Investigaciones Neurológicas "Raúl Carrea"; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
description INTRODUCTION: Adenosine A2A receptors are localized in the brain, mainly within the caudate and putamen nuclei of the basal ganglia. Their activation leads to stimulation of the 'indirect' pathway. Conversely, administration of A2A receptor antagonists leads to inhibition of this pathway, which was translated into reduced hypomotility in several animal models of parkinsonism. AREAS COVERED: In this review, the effects of two A2A receptor antagonists, istradefylline and tozadenant, on parkinsonian symptoms in animal and humans will be discussed. EXPERT OPINION: Animal studies have shown potent antiparkinsonian effects for several A2A receptor antagonists, including istradefylline. In clinical trials, istradefylline reduced OFF time when administered with levodopa, but results are inconclusive. Results with tozadenant are scarce. Modification of thalamic blood flow compatible with reduced inhibition was noted in one small trial, followed by a significant reduction in OFF time in a larger one. Therefore, both drugs show promising efficacy for the reduction of OFF time in levodopa-treated Parkinson's disease patients, but further research is needed in order to obtain definitive conclusions.
publishDate 2014
dc.date.none.fl_str_mv 2014-03
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
http://purl.org/coar/resource_type/c_6501
info:ar-repo/semantics/articulo
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv http://hdl.handle.net/11336/16826
Perez Lloret, Santiago; Merello, Marcelo Jorge; Two new adenosine receptor antagonists for the treatment of Parkinson's disease: istradefylline versus tozadenant; Taylor & Francis; Expert Opinion On Pharmacotherapy; 15; 8; 3-2014; 1097-1107
1465-6566
1744-7666
url http://hdl.handle.net/11336/16826
identifier_str_mv Perez Lloret, Santiago; Merello, Marcelo Jorge; Two new adenosine receptor antagonists for the treatment of Parkinson's disease: istradefylline versus tozadenant; Taylor & Francis; Expert Opinion On Pharmacotherapy; 15; 8; 3-2014; 1097-1107
1465-6566
1744-7666
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/url/http://www.tandfonline.com/doi/abs/10.1517/14656566.2014.903924?journalCode=ieop20
info:eu-repo/semantics/altIdentifier/doi/10.1517/14656566.2014.903924
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
eu_rights_str_mv openAccess
rights_invalid_str_mv https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.format.none.fl_str_mv application/pdf
application/pdf
dc.publisher.none.fl_str_mv Taylor & Francis
publisher.none.fl_str_mv Taylor & Francis
dc.source.none.fl_str_mv reponame:CONICET Digital (CONICET)
instname:Consejo Nacional de Investigaciones Científicas y Técnicas
reponame_str CONICET Digital (CONICET)
collection CONICET Digital (CONICET)
instname_str Consejo Nacional de Investigaciones Científicas y Técnicas
repository.name.fl_str_mv CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicas
repository.mail.fl_str_mv dasensio@conicet.gov.ar; lcarlino@conicet.gov.ar
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score 12.637756

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