BCI-838, an orally active mGluR2/3 receptor antagonist pro-drug, rescues learning behavior deficits in the PS19 MAPT

Male Mice Humans Animals Prodrugs / therapeutic use Tauopathies / pathology tau Proteins / genetics Receptors, Metabotropic Glutamate Alzheimer Disease / pathology Mice, Transgenic Disease Models, Animal
BCI-838 Frontotemporal dementia Metabotropic glutamate receptors 2/3 Tauopathy Transgenic mice microtubule associated protein tau (MAPT)

Journal

Neuroscience letters
ISSN: 1872-7972
Titre abrégé: Neurosci Lett
Pays: Ireland
ID NLM: 7600130

Informations de publication

Date de publication:
16 02 2023
Historique:
received: 27 11 2022
revised: 04 01 2023
accepted: 12 01 2023
pmc-release: 16 02 2024
pubmed: 20 1 2023
medline: 25 2 2023
entrez: 19 1 2023
Statut: ppublish

Résumé

Tauopathies are a heterogeneous group of neurodegenerative disorders that are clinically and pathologically distinct from Alzheimer's disease (AD) having tau inclusions in neurons and/or glia as their most prominent neuropathological feature. BCI-838 (MGS00210) is a group II metabotropic glutamate receptor (mGluR2/3) antagonist pro-drug. Previously, we reported that orally administered BCI-838 improved learning behavior and reduced anxiety in Dutch (APP

Identifiants

DOI: 10.1016/j.neulet.2023.137080 PMID: 36657633 PMC: PMC9974759
pubmed: 36657633
pii: S0304-3940(23)00034-4
doi: 10.1016/j.neulet.2023.137080
pmc: PMC9974759
mid: NIHMS1866858
pii:
doi:

Substances chimiques

BCI-838 0
metabotropic glutamate receptor 2 0
Prodrugs 0
tau Proteins 0
Receptors, Metabotropic Glutamate 0
MAPT protein, human 0
Mapt protein, mouse 0

Types de publication

Journal Article Research Support, N.I.H., Extramural Research Support, U.S. Gov't, Non-P.H.S.

Langues

eng

Sous-ensembles de citation

IM

Pagination

137080

Subventions

Organisme : RRD VA
ID : I01 RX002333
Pays : United States
Organisme : NIA NIH HHS
ID : P30 AG072980
Pays : United States
Organisme : RRD VA
ID : I21 RX003459
Pays : United States
Organisme : RRD VA
ID : I01 RX000684
Pays : United States
Organisme : NIA NIH HHS
ID : P30 AG019610
Pays : United States
Organisme : BLRD VA
ID : I01 BX004067
Pays : United States
Organisme : RRD VA
ID : I01 RX002660
Pays : United States
Organisme : NIA NIH HHS
ID : P30 AG066514
Pays : United States
Organisme : RRD VA
ID : I01 RX003846
Pays : United States

Informations de copyright

Published by Elsevier B.V.

Déclaration de conflit d'intérêts

Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

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Auteurs

Georgina Perez-Garcia (G)

Department of Neurology, Icahn School of Medicine at Mount Sinai, New York, NY 10029, USA; Research and Development, James J. Peters Veterans Affairs Medical Center, Bronx, NY 10468, USA.

Mesude Bicak (M)

Department of Genetics and Genomic Sciences, Icahn School of Medicine at Mount Sinai, New York, NY 10029, USA; Hasso Plattner Institute for Digital Health at Mount Sinai, Icahn School of Medicine at Mount Sinai, New York, NY 10029, USA.

Jean-Vianney Haure-Mirande (JV)

Department of Neurology, Icahn School of Medicine at Mount Sinai, New York, NY 10029, USA.

Gissel M Perez (GM)

Research and Development, James J. Peters Veterans Affairs Medical Center, Bronx, NY 10468, USA.

Alena Otero-Pagan (A)

Research and Development, James J. Peters Veterans Affairs Medical Center, Bronx, NY 10468, USA.

Miguel A Gama Sosa (MA)

Department of Psychiatry, Icahn School of Medicine at Mount Sinai, New York, NY 10029, USA; General Medical Research Service, James J. Peters Department of Veterans Affairs Medical Center, Bronx, NY 10468, USA.

Rita De Gasperi (R)

Research and Development, James J. Peters Veterans Affairs Medical Center, Bronx, NY 10468, USA; Department of Psychiatry, Icahn School of Medicine at Mount Sinai, New York, NY 10029, USA.

Mary Sano (M)

Research and Development, James J. Peters Veterans Affairs Medical Center, Bronx, NY 10468, USA; Department of Psychiatry, Icahn School of Medicine at Mount Sinai, New York, NY 10029, USA; Mount Sinai Alzheimer's Disease Research Center and Ronald M. Loeb Center for Alzheimer's Disease, Icahn School of Medicine at Mount Sinai, New York, NY 10029, USA.

Carrolee Barlow (C)

BrainCells Inc., La Jolla, CA 92037, USA; EScape Bio, South San Francisco, CA 94080, USA.

Fred H Gage (FH)

BrainCells Inc., La Jolla, CA 92037, USA; Laboratory of Genetics, The Salk Institute for Biological Studies, La Jolla, CA 92037, USA.

Benjamin Readhead (B)

Arizona State University-Banner Neurodegenerative Disease Research Center, Arizona State University, Tempe, AZ 85287, USA.

Michelle E Ehrlich (ME)

Department of Neurology, Icahn School of Medicine at Mount Sinai, New York, NY 10029, USA; Department of Genetics and Genomic Sciences, Icahn School of Medicine at Mount Sinai, New York, NY 10029, USA.

Sam Gandy (S)

Department of Neurology, Icahn School of Medicine at Mount Sinai, New York, NY 10029, USA; Research and Development, James J. Peters Veterans Affairs Medical Center, Bronx, NY 10468, USA; Department of Psychiatry, Icahn School of Medicine at Mount Sinai, New York, NY 10029, USA; Mount Sinai Alzheimer's Disease Research Center and Ronald M. Loeb Center for Alzheimer's Disease, Icahn School of Medicine at Mount Sinai, New York, NY 10029, USA; Mount Sinai Center for Cognitive Health, Icahn School of Medicine at Mount Sinai, New York, NY 10029, USA.

Gregory A Elder (GA)

Department of Neurology, Icahn School of Medicine at Mount Sinai, New York, NY 10029, USA; Department of Psychiatry, Icahn School of Medicine at Mount Sinai, New York, NY 10029, USA; Mount Sinai Alzheimer's Disease Research Center and Ronald M. Loeb Center for Alzheimer's Disease, Icahn School of Medicine at Mount Sinai, New York, NY 10029, USA; Neurology Service, James J. Peters Veterans Affairs Medical Center, Bronx, NY 10468, USA. Electronic address: gregory.elder@mssm.edu.

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Classifications MeSH

questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › BCI-838, an orally active mGluR2/3 receptor...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › BCI-838, an orally active mGluR2/3 receptor...
questionsmedicales.fr › Eucaryotes › Animaux › BCI-838, an orally active mGluR2/3 receptor...
questionsmedicales.fr › Préparations pharmaceutiques › Promédicaments › BCI-838, an orally active mGluR2/3 receptor...
questionsmedicales.fr › Maladies du système nerveux › Maladies neurodégénératives › Tauopathies › BCI-838, an orally active mGluR2/3 receptor...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines de tissu nerveux › Protéines associées aux microtubules › Protéines tau › BCI-838, an orally active mGluR2/3 receptor...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines membranaires › Récepteurs de surface cellulaire › Récepteurs aux neuromédiateurs › Récepteurs aux acides aminés › Récepteurs au glutamate › Récepteurs métabotropes au glutamate › BCI-838, an orally active mGluR2/3 receptor...
questionsmedicales.fr › Troubles mentaux › Troubles neurocognitifs › Démence › Maladie d'Alzheimer › BCI-838, an orally active mGluR2/3 receptor...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › Souris transgéniques › BCI-838, an orally active mGluR2/3 receptor...
questionsmedicales.fr › Techniques d'investigation › Modèles théoriques › Modèles biologiques › Modèles animaux de maladie humaine › BCI-838, an orally active mGluR2/3 receptor...