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AB120008

MPEP hydrochloride, mGlu5 antagonist

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(34 Publications)

MW 229.7 Da, Purity >99%. Subtype selective and potent non-competitive mGlu5 antagonist (IC50 = 36 nM). Central effects following systemic administration in vivo.

View Alternative Names

GLUR, GPRC1E, GRM5_HUMAN, Glutamate receptor metabotropic 5, Metabotropic glutamate receptor 5, Metabotropic glutamate receptor 5 variant F, Metabotropic glutamate receptor 5 variant G, Metabotropic glutamate receptor 5 variant H, PPP1R86, Protein phosphatase 1 regulatory subunit 86, Smp_128940, mGlu5, mGluR5

4 Images
Functional Studies - MPEP hydrochloride, mGlu5 antagonist (AB120008)
  • FuncS

Unknown

Functional Studies - MPEP hydrochloride, mGlu5 antagonist (AB120008)

Basal PLD activity is strongly stimulated by the D1/5R agonist and blocked by the D1/5R, mGluR5, mGluR1, and the PLD-linked mGluR antagonists in the amygdala of cocaine CPP animals.
The dotted line indicates PLD activity associated with control slices (no EtOH added) which was determined for each animal and used to calculate the change in PLD activity levels with EtOH and/or drug application.

Image from Krishnan B, et al. Plos One, 6(9), e25639. Fig 7,; doi: 10.1371/journal.pone.0025639

Functional Studies - MPEP hydrochloride, mGlu5 antagonist (AB120008)
  • FuncS

PubMed

Functional Studies - MPEP hydrochloride, mGlu5 antagonist (AB120008)

Ca2+ signal from a field A neuron, a field B neuron, and field A astrocytes in response to repetitive episodes of NMDA stimulation (black arrowheads). The NMDA stimulation that evoked an ictal discharge became ineffective after blocking the astrocyte response by bath perfusion with MPEP (ab120008) and PPADS (ab120009). An ictal discharge could be recovered by increasing the number of NMDA puffs (white arrowheads). A double NMDA pulse evoked both astrocyte activation and the ictal discharge after inhibitor washout.

Image from Gómez-Gonzalo M et al., PLoS Biol. 2010;8(4):e1000352. Fig 6(A).; doi: 10.1371/journal.pbio.1000352.

Functional Studies - MPEP hydrochloride, mGlu5 antagonist (AB120008)
  • FuncS

PubMed

Functional Studies - MPEP hydrochloride, mGlu5 antagonist (AB120008)

Astrocyte Ca2+ signal inhibition does not affect interictal discharges. (A–D) Mean percentage of astrocytes activated by the ictal discharges (A), mean duration (B) and frequency (C) of the ictal discharge, and mean frequency of interictal discharges (D) under different experimental conditions in EC slice preparations. Controls (n=16), MPEP (ab120008) (n=7), PPADS (ab120009) (n=9), and MPEP+PPADS (n=3). A single asterisk (*) indicates p<0.05; double asterisks (**), p<0.01.

Image from Gómez-Gonzalo M et al., PLoS Biol. 2010;8(4):e1000352. Fig 2.; doi: 10.1371/journal.pbio.1000352. Reproduced under the Creative Commons license http://creativecommons.org/licenses/by/4.0/

Chemical Structure - MPEP hydrochloride, mGlu5 antagonist (AB120008)
  • Chemical Structure

Lab

Chemical Structure - MPEP hydrochloride, mGlu5 antagonist (AB120008)

2D chemical structure image of ab120008, MPEP hydrochloride, mGlu5 antagonist

Key facts

CAS number

219911-35-0

Purity

>99%

Form

Solid

form

Molecular weight

229.7 Da

Molecular formula

C<sub>1</sub><sub>4</sub>H<sub>1</sub><sub>2</sub>ClN

PubChem

9794588

Nature

Synthetic

Solubility

Soluble in water to 5 mM, in ethanol to 100 mM and in DMSO to 100 mM

Biochemical name

MPEP hydrochloride

Biological description

Subtype selective and potent non-competitive mGlu5 antagonist (IC50 = 36 nM). Central effects following systemic administration in vivo.

Canonical smiles

CC1=NC(=CC=C1)C#CC2=CC=CC=C2.Cl

InChi

InChI=1S/C14H11N.ClH/c1-12-6-5-9-14(15-12)11-10-13-7-3-2-4-8-13;/h2-9H,1H3;1H

InChiKey

PKDHDJBNEKXCBI-UHFFFAOYSA-N

IUPAC Name

2-methyl-6-(2-phenylethynyl)pyridine;hydrochloride

Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
+4°C
Appropriate long-term storage conditions
+4°C
Storage information
Store under desiccating conditions|The product can be stored for up to 12 months

Product protocols

Publications (34)

Recent publications for all applications. Explore the full list and refine your search

Journal of neuroscience research 101:1170-1187 PubMed36807930

2023

Metabotropic glutamate receptor 5-mediated inhibition of inward-rectifying K channel 4.1 contributes to orofacial ectopic mechanical allodynia following inferior alveolar nerve transection in male mice.

Applications

Unspecified application

Species

Unspecified reactive species

Yi-Ke Li,Yan-Yan Zhang,Jiu Lin,Ya-Jing Liu,Yue-Ling Li,Yu-Heng Feng,Jia-Shuo Zhao,Cheng Zhou,Fei Liu,Jie-Fei Shen

The Journal of neuroscience : the official journal of the Society for Neuroscience 42:6211-6220 PubMed35790402

2022

Induction of Activity-Dependent Plasticity at Auditory Nerve Synapses.

Applications

Unspecified application

Species

Unspecified reactive species

Nicole F Wong,Matthew A Xu-Friedman

Biology of reproduction 107:916-927 PubMed35746896

2022

Glutamate can act as a signaling molecule in mouse preimplantation embryos†.

Applications

Unspecified application

Species

Unspecified reactive species

Alexandra Špirková,Veronika Kovaříková,Zuzana Šefčíková,Jozef Pisko,Martina Kšiňanová,Juraj Koppel,Dušan Fabian,Štefan Čikoš

eLife 8: PubMed31535971

2019

ON selectivity in the visual system is a multisynaptic process involving both glutamatergic and GABAergic inhibition.

Applications

Unspecified application

Species

Unspecified reactive species

Sebastian Molina-Obando,Juan Felipe Vargas-Fique,Miriam Henning,Burak Gür,T Moritz Schladt,Junaid Akhtar,Thomas K Berger,Marion Silies

Scientific reports 8:4407 PubMed29535347

2018

Direct coupling of detergent purified human mGlu receptor to the heterotrimeric G proteins Gq and Gs.

Applications

Unspecified application

Species

Unspecified reactive species

Chady Nasrallah,Karine Rottier,Romain Marcellin,Vincent Compan,Joan Font,Amadeu Llebaria,Jean-Philippe Pin,Jean-Louis Banères,Guillaume Lebon

Scientific reports 7:44817 PubMed28322255

2017

Ca-permeable AMPA receptors in mouse olfactory bulb astrocytes.

Applications

Unspecified application

Species

Unspecified reactive species

Damian Droste,Gerald Seifert,Laura Seddar,Oliver Jädtke,Christian Steinhäuser,Christian Lohr

Frontiers in cellular neuroscience 10:252 PubMed27872582

2016

Separate Ionotropic and Metabotropic Glutamate Receptor Functions in Depotentiation vs. LTP: A Distinct Role for Group1 mGluR Subtypes and NMDARs.

Applications

Unspecified application

Species

Unspecified reactive species

Amira Latif-Hernandez,Enrico Faldini,Tariq Ahmed,Detlef Balschun

Scientific reports 6:28454 PubMed27345695

2016

Layer-specific potentiation of network GABAergic inhibition in the CA1 area of the hippocampus.

Applications

Unspecified application

Species

Unspecified reactive species

Michelangelo Colavita,Geoffrey Terral,Clement E Lemercier,Filippo Drago,Giovanni Marsicano,Federico Massa

Frontiers in cellular neuroscience 9:345 PubMed26388733

2015

Differential expression of metabotropic glutamate and GABA receptors at neocortical glutamatergic and GABAergic axon terminals.

Applications

Unspecified application

Species

Unspecified reactive species

Luca Bragina,Tiziana Bonifacino,Silvia Bassi,Marco Milanese,Giambattista Bonanno,Fiorenzo Conti

Journal of neurophysiology 113:3634-45 PubMed25855696

2015

Different pools of glutamate receptors mediate sensitivity to ambient glutamate in the cochlear nucleus.

Applications

Unspecified application

Species

Unspecified reactive species

Yang Yang,Matthew A Xu-Friedman
View all publications

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