Therapeutic Potential of Kainate Receptors
Glutamate receptors are key mediators of brain communication. Among ionotropic glutamate receptors, kainate receptors (KARs) have been least explored and their relevance to pathophysiology is relatively obscure. This is in part due to the relatively low abundance of KARs, the regulatory function in...
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| Format: | Online |
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Blackwell Publishing Ltd
2011
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| Online Access: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3430855/ |
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pubmed-3430855 |
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pubmed-34308552012-08-30 Therapeutic Potential of Kainate Receptors Matute, Carlos Reviews Glutamate receptors are key mediators of brain communication. Among ionotropic glutamate receptors, kainate receptors (KARs) have been least explored and their relevance to pathophysiology is relatively obscure. This is in part due to the relatively low abundance of KARs, the regulatory function in network activity they play, the lack of specific agonists and antagonists for this receptor subtype, as well as to the absence of striking phenotypes in mice deficient in KAR subunits. Nonetheless, it is now well established that KARs are located presynaptically whereby they regulate glutamate and GABA release, and thus, excitability and participate in short-term plasticity. In turn, KARs are also located postsynaptically and their activation contributes to synaptic integration. The development of specific novel ligands is helping to further investigate the contribution of KARs to health and disease. In this review, I summarize current knowledge about KAR physiology and pharmacology, and discuss their involvement in cell death and disease. In addition, I recapitulate the available data about the use of KAR antagonists and receptor subunit deficient mice in experimental paradigms of brain diseases, as well as the main findings about KAR roles in human CNS disorders. In sum, subunit specific antagonists have therapeutic potential in neurodegenerative and psychiatric diseases as well as in epilepsy and pain. Knowledge about the genetics of KARs will also help to understand the pathophysiology of those and other illnesses. Blackwell Publishing Ltd 2011-12 2010-12-06 /pmc/articles/PMC3430855/ /pubmed/21129167 http://dx.doi.org/10.1111/j.1755-5949.2010.00204.x Text en © 2010 Blackwell Publishing Ltd http://creativecommons.org/licenses/by/2.5/ Re-use of this article is permitted in accordance with the Creative Commons Deed, Attribution 2.5, which does not permit commercial exploitation. |
| repository_type |
Open Access Journal |
| institution_category |
Foreign Institution |
| institution |
US National Center for Biotechnology Information |
| building |
NCBI PubMed |
| collection |
Online Access |
| language |
English |
| format |
Online |
| author |
Matute, Carlos |
| spellingShingle |
Matute, Carlos Therapeutic Potential of Kainate Receptors |
| author_facet |
Matute, Carlos |
| author_sort |
Matute, Carlos |
| title |
Therapeutic Potential of Kainate Receptors |
| title_short |
Therapeutic Potential of Kainate Receptors |
| title_full |
Therapeutic Potential of Kainate Receptors |
| title_fullStr |
Therapeutic Potential of Kainate Receptors |
| title_full_unstemmed |
Therapeutic Potential of Kainate Receptors |
| title_sort |
therapeutic potential of kainate receptors |
| description |
Glutamate receptors are key mediators of brain communication. Among ionotropic glutamate receptors, kainate receptors (KARs) have been least explored and their relevance to pathophysiology is relatively obscure. This is in part due to the relatively low abundance of KARs, the regulatory function in network activity they play, the lack of specific agonists and antagonists for this receptor subtype, as well as to the absence of striking phenotypes in mice deficient in KAR subunits. Nonetheless, it is now well established that KARs are located presynaptically whereby they regulate glutamate and GABA release, and thus, excitability and participate in short-term plasticity. In turn, KARs are also located postsynaptically and their activation contributes to synaptic integration. The development of specific novel ligands is helping to further investigate the contribution of KARs to health and disease. In this review, I summarize current knowledge about KAR physiology and pharmacology, and discuss their involvement in cell death and disease. In addition, I recapitulate the available data about the use of KAR antagonists and receptor subunit deficient mice in experimental paradigms of brain diseases, as well as the main findings about KAR roles in human CNS disorders. In sum, subunit specific antagonists have therapeutic potential in neurodegenerative and psychiatric diseases as well as in epilepsy and pain. Knowledge about the genetics of KARs will also help to understand the pathophysiology of those and other illnesses. |
| publisher |
Blackwell Publishing Ltd |
| publishDate |
2011 |
| url |
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3430855/ |
| _version_ |
1611553220627267584 |