ParkinsonFranceV1, Main, Exploration, bibRecord, 000771

The mGluR5 negative allosteric modulator dipraglurant reduces dyskinesia in the MPTP macaque model

Identifieur interne : 000771 ( Main/Exploration ); précédent : 000770; suivant : 000772

The mGluR5 negative allosteric modulator dipraglurant reduces dyskinesia in the MPTP macaque model

Auteurs : Erwan Bezard [France] ; Elsa Y. Pioli [Royaume-Uni] ; Qin Li [Royaume-Uni] ; Françoise Girard [France] ; Vincent Mutel [Suisse] ; Charlotte Keywood [Suisse] ; Francois Tison [France] ; Olivier Rascol [France] ; Sonia M. Poli [Italie]

Source :

Movement Disorders [ 0885-3185 ] ; 2014-07.

RBID : Hal:hal-01288050

Abstract

BACKGROUND:Blocking metabotropic glutamate receptor type 5 (mGluR5) has been proposed as a target for levodopa-induced dyskinesias (LID) in Parkinson's disease (PD). We assessed the effect on LID of dipraglurant, a potent selective mGluR5 receptor negative allosteric modulator in the gold-standard LID macaque model.METHODS:Dipraglurant (3, 10, and 30 mg/kg, by mouth) was tested in the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) macaque model of LID in a four-way crossover, single-dose, controlled study (n = 8).RESULTS:Dipraglurant inhibited dyskinesias in the LID macaque model, with best effect reached at 30 mg/kg dose with no alteration of levodopa efficacy.CONCLUSION:Acute challenges of dipraglurant were efficacious on choreic and dystonic LID in the MPTP-macaque model. Dipraglurant pharmacokinetic variables were similar to those of levodopa, suggesting that both drugs can be co-administered simultaneously in further studies.

Url:

https://hal.archives-ouvertes.fr/hal-01288050

DOI: 10.1002/mds.25920

Affiliations:

Links toward previous steps (curation, corpus...)

to stream Hal, to step Corpus: 000B35
to stream Hal, to step Curation: 000B35
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Le document en format XML

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<country>Italie</country>
</affiliation>
</author>
</analytic>
<idno type="DOI">10.1002/mds.25920</idno>
<series><title level="j">Movement Disorders</title>
<idno type="ISSN">0885-3185</idno>
<imprint><date type="datePub">2014-07</date>
</imprint>
</series>
</biblStruct>
</sourceDesc>
</fileDesc>
<profileDesc><textClass></textClass>
</profileDesc>
</teiHeader>
<front><div type="abstract" xml:lang="en">BACKGROUND:Blocking metabotropic glutamate receptor type 5 (mGluR5) has been proposed as a target for levodopa-induced dyskinesias (LID) in Parkinson's disease (PD). We assessed the effect on LID of dipraglurant, a potent selective mGluR5 receptor negative allosteric modulator in the gold-standard LID macaque model.METHODS:Dipraglurant (3, 10, and 30 mg/kg, by mouth) was tested in the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) macaque model of LID in a four-way crossover, single-dose, controlled study (n = 8).RESULTS:Dipraglurant inhibited dyskinesias in the LID macaque model, with best effect reached at 30 mg/kg dose with no alteration of levodopa efficacy.CONCLUSION:Acute challenges of dipraglurant were efficacious on choreic and dystonic LID in the MPTP-macaque model. Dipraglurant pharmacokinetic variables were similar to those of levodopa, suggesting that both drugs can be co-administered simultaneously in further studies.</div>
</front>
</TEI>
<affiliations><list><country><li>France</li>
<li>Italie</li>
<li>Royaume-Uni</li>
<li>Suisse</li>
</country>
<region><li>Aquitaine</li>
<li>Nouvelle-Aquitaine</li>
</region>
<settlement><li>Bordeaux</li>
</settlement>
<orgName><li>Université de Bordeaux</li>
</orgName>
</list>
<tree><country name="France"><region name="Nouvelle-Aquitaine"><name sortKey="Bezard, Erwan" sort="Bezard, Erwan" uniqKey="Bezard E" first="Erwan" last="Bezard">Erwan Bezard</name>
</region>
<name sortKey="Girard, Francoise" sort="Girard, Francoise" uniqKey="Girard F" first="Françoise" last="Girard">Françoise Girard</name>
<name sortKey="Rascol, Olivier" sort="Rascol, Olivier" uniqKey="Rascol O" first="Olivier" last="Rascol">Olivier Rascol</name>
<name sortKey="Tison, Francois" sort="Tison, Francois" uniqKey="Tison F" first="Francois" last="Tison">Francois Tison</name>
</country>
<country name="Royaume-Uni"><noRegion><name sortKey="Pioli, Elsa Y" sort="Pioli, Elsa Y" uniqKey="Pioli E" first="Elsa Y." last="Pioli">Elsa Y. Pioli</name>
</noRegion>
<name sortKey="Li, Qin" sort="Li, Qin" uniqKey="Li Q" first="Qin" last="Li">Qin Li</name>
</country>
<country name="Suisse"><noRegion><name sortKey="Mutel, Vincent" sort="Mutel, Vincent" uniqKey="Mutel V" first="Vincent" last="Mutel">Vincent Mutel</name>
</noRegion>
<name sortKey="Keywood, Charlotte" sort="Keywood, Charlotte" uniqKey="Keywood C" first="Charlotte" last="Keywood">Charlotte Keywood</name>
</country>
<country name="Italie"><noRegion><name sortKey="Poli, Sonia M" sort="Poli, Sonia M" uniqKey="Poli S" first="Sonia M." last="Poli">Sonia M. Poli</name>
</noRegion>
</country>
</tree>
</affiliations>
</record>

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	La maladie de Parkinson en France (serveur d'exploration)
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La maladie de Parkinson en France (serveur d'exploration)

The mGluR5 negative allosteric modulator dipraglurant reduces dyskinesia in the MPTP macaque model

The mGluR5 negative allosteric modulator dipraglurant reduces dyskinesia in the MPTP macaque model

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