2-Methyl-6-(phenylethynyl)pyridine Hydrochloride Modulates Metabotropic Glutamate 5 Receptors Endogenously Expressed in Zebrafish Brain
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Title
2-Methyl-6-(phenylethynyl)pyridine Hydrochloride Modulates Metabotropic Glutamate 5 Receptors Endogenously Expressed in Zebrafish BrainAuthor (s)
Date
2016-12-21Publisher
American Chemical SocietyISSN
1948-7193Bibliographic citation
Albasanz, J. L., Santana, S., Guzman-Sanchez, F., León, D., Burgos, J. S., and Martín, M. (2016) 2-Methyl-6-(phenylethynyl)pyridine Hydrochloride Modulates Metabotropic Glutamate 5 Receptors Endogenously Expressed in Zebrafish Brain. ACS Chem. Neurosci. , 7, 12, 1690-1697 DOI: 10.1021/acschemneuro.6b00213Type
info:eu-repo/semantics/articlePublisher version
https://pubs.acs.org/doi/full/10.1021/acschemneuro.6b00213Version
info:eu-repo/semantics/acceptedVersionSubject
Abstract
Due to phylogenetic proximity to the human, zebrafish has been recognized as a reliable model to study Alzheimer’s disease (AD) and other central nervous system disorders. Furthermore, metabotropic glutamate receptors ... [+]
Due to phylogenetic proximity to the human, zebrafish has been recognized as a reliable model to study Alzheimer’s disease (AD) and other central nervous system disorders. Furthermore, metabotropic glutamate receptors have been previously reported to be impaired in brain from AD patients. Metabotropic glutamate 5 (mGlu5) receptors are G-protein coupled receptors proposed as potential targets for therapy of different neurodegenerative disorders. Thus, MPEP (2-methyl-6-(phenylethynyl)pyridine hydrochloride), a selective noncompetitive mGlu5 receptor antagonist, has been suggested for pharmacological treatment of AD. The aim of the present work was to quantify mGlu5 receptors in brain from zebrafish and to study the possible modulation of these receptors by MPEP treatment. To this end, radioligand binding assay and open field test were used. Results showed a slightly higher presence of mGlu5 receptors in brain from male than in that from female zebrafish. However, a significant increase of mGlu5 receptor in male without variation in female was observed after MPEP treatment. This gender specific response was also observed in locomotor behavior, being significantly decreased only in male zebrafish. These results confirm the presence of mGlu5 receptors in brain from zebrafish and their gender specific modulation by selective antagonist treatment and suggest a role of these receptors on locomotor activity, which is affected in many disorders. In addition, our data point to zebrafish as a useful model to study mGlu receptor function in both healthy and pathological conditions. [-]
Is part of
ACS Chemical Neuroscience, 2016, vol. 7, no 12Funder Name
Ministerio de Economía y Competitividad (España)
Funder ID
http://dx.doi.org/10.13039/501100004837
Project code
BFU2011-23034 | PEII-2014-030-P
Project title or grant
Control de la neuromodulación de las vías mediadas por los receptores de adenosina y metabotrópicos de glutamato: potencial terapéutico en enfermedades neurodegenerativas | Regulación de receptores de adenosina y
metabotrópicos de glutamato durante el envejecimiento:
implicación en procesos de degeneración y muerte
celular.
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info:eu-repo/semantics/openAccess
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- MED_Articles [657]