Past, present and future of A(2A) adenosine receptor antagonists in the therapy of Parkinson's disease.ents. Correlates with Alzheimer 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...
| Main Authors: | , , , , , |
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| Format: | info:eu-repo/semantics/article |
| Language: | eng |
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Pergamon Elsevier Science LTD
2012
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| Subjects: | |
| Online Access: | https://hdl.handle.net/10171/22827 |
| _version_ | 1793400052917469184 |
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| author | Armentero, M.T. (Marie Therese) Pinna, A. (Annalisa) Ferre, S. (Sergi) Lanciego, J.L. (José Luis) Müller, C.E. (Christa E.) Franco, R. (Rafael) |
| author_facet | Armentero, M.T. (Marie Therese) Pinna, A. (Annalisa) Ferre, S. (Sergi) Lanciego, J.L. (José Luis) Müller, C.E. (Christa E.) Franco, R. (Rafael) |
| author_sort | Armentero, M.T. (Marie Therese) |
| collection | DSpace |
| 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. |
| format | info:eu-repo/semantics/article |
| id | oai:dadun.unav.edu:10171-22827 |
| institution | Universidad de Navarra |
| language | eng |
| publishDate | 2012 |
| publisher | Pergamon Elsevier Science LTD |
| record_format | dspace |
| spelling | oai:dadun.unav.edu:10171-228272017-05-13T23:34:38Z Past, present and future of A(2A) adenosine receptor antagonists in the therapy of Parkinson's disease.ents. Correlates with Alzheimer disease Armentero, M.T. (Marie Therese) Pinna, A. (Annalisa) Ferre, S. (Sergi) Lanciego, J.L. (José Luis) Müller, C.E. (Christa E.) Franco, R. (Rafael) Basal ganglia Receptor heteromer Heteromer-selective antagonist Neuroprotection Postsynaptic heteromer Presynaptic heteromer 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. 2012-07-04T10:34:28Z 2012-07-04T10:34:28Z 2011-12 info:eu-repo/semantics/article https://hdl.handle.net/10171/22827 eng info:eu-repo/semantics/closedAccess Pergamon Elsevier Science LTD |
| spellingShingle | Basal ganglia Receptor heteromer Heteromer-selective antagonist Neuroprotection Postsynaptic heteromer Presynaptic heteromer Armentero, M.T. (Marie Therese) Pinna, A. (Annalisa) Ferre, S. (Sergi) Lanciego, J.L. (José Luis) Müller, C.E. (Christa E.) Franco, R. (Rafael) Past, present and future of A(2A) adenosine receptor antagonists in the therapy of Parkinson's disease.ents. Correlates with Alzheimer disease |
| title | Past, present and future of A(2A) adenosine receptor antagonists in the therapy of Parkinson's disease.ents. Correlates with Alzheimer disease |
| title_full | Past, present and future of A(2A) adenosine receptor antagonists in the therapy of Parkinson's disease.ents. Correlates with Alzheimer disease |
| title_fullStr | Past, present and future of A(2A) adenosine receptor antagonists in the therapy of Parkinson's disease.ents. Correlates with Alzheimer disease |
| title_full_unstemmed | Past, present and future of A(2A) adenosine receptor antagonists in the therapy of Parkinson's disease.ents. Correlates with Alzheimer disease |
| title_short | Past, present and future of A(2A) adenosine receptor antagonists in the therapy of Parkinson's disease.ents. Correlates with Alzheimer disease |
| title_sort | past, present and future of a(2a) adenosine receptor antagonists in the therapy of parkinson's disease.ents. correlates with alzheimer disease |
| topic | Basal ganglia Receptor heteromer Heteromer-selective antagonist Neuroprotection Postsynaptic heteromer Presynaptic heteromer |
| url | https://hdl.handle.net/10171/22827 |
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