MPEP hydrochloride, mGlu5 antagonist (ab120008)
Key features and details
- Potent, selective mGlu5 antagonist
- CAS Number: 219911-35-0
- Purity: > 99%
- Soluble in water to 5 mM, in ethanol to 100 mM and in DMSO to 100 mM
- Form / State: Solid
- Source: Synthetic
Overview
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Product name
MPEP hydrochloride, mGlu5 antagonist -
Description
Potent, selective mGlu5 antagonist -
Biological description
Subtype selective and potent non-competitive mGlu5 antagonist (IC50 = 36 nM). Central effects following systemic administration in vivo.
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Purity
> 99% -
CAS Number
219911-35-0 -
Chemical structure
Properties
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Chemical name
2-Methyl-6-(phenylethynyl)pyridine hydrochloride -
Molecular weight
229.71 -
Molecular formula
C14H11N.HCl -
PubChem identifier
9794588 -
Storage instructions
Store at +4°C. Store under desiccating conditions. The product can be stored for up to 12 months. -
Solubility overview
Soluble in water to 5 mM, in ethanol to 100 mM and in DMSO to 100 mM -
Handling
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
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SMILES
[Cl-].Cc2cccc(C#Cc1ccccc1)[nH+]2 -
Source
Synthetic
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Research areas
Images
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Chemical Structure - MPEP hydrochloride, mGlu5 antagonist (ab120008)2D chemical structure image of ab120008, MPEP hydrochloride, mGlu5 antagonist
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Functional Studies - MPEP hydrochloride, mGlu5 antagonist (ab120008)Image from Krishnan B, et al. Plos One, 6(9), e25639. Fig 7,; doi: 10.1371/journal.pone.0025639Basal 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. -
Functional Studies - MPEP hydrochloride, mGlu5 antagonist (ab120008)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/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. -
Functional Studies - MPEP hydrochloride, mGlu5 antagonist (ab120008)Image from Gómez-Gonzalo M et al., PLoS Biol. 2010;8(4):e1000352. Fig 6(A).; doi: 10.1371/journal.pbio.1000352.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.
Protocols
To our knowledge, customised protocols are not required for this product. Please try the standard protocols listed below and let us know how you get on.
References (31)
ab120008 has been referenced in 31 publications.
- Molina-Obando S et al. ON selectivity in the Drosophila visual system is a multisynaptic process involving both glutamatergic and GABAergic inhibition. Elife 8:N/A (2019). PubMed: 31535971
- Nasrallah C et al. Direct coupling of detergent purified human mGlu5 receptor to the heterotrimeric G proteins Gq and Gs. Sci Rep 8:4407 (2018). PubMed: 29535347
- Droste D et al. Ca2+-permeable AMPA receptors in mouse olfactory bulb astrocytes. Sci Rep 7:44817 (2017). PubMed: 28322255
- Latif-Hernandez A et al. Separate Ionotropic and Metabotropic Glutamate Receptor Functions in Depotentiation vs. LTP: A Distinct Role for Group1 mGluR Subtypes and NMDARs. Front Cell Neurosci 10:252 (2016). PubMed: 27872582
- Colavita M et al. Layer-specific potentiation of network GABAergic inhibition in the CA1 area of the hippocampus. Sci Rep 6:28454 (2016). PubMed: 27345695
