MPEP hydrochloride，mGlu5拮抗剂(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
概述
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产品名称
MPEP hydrochloride，mGlu5拮抗剂 -
描述
Potent，selective mGlu5拮抗剂 -
生物学描述
Subtype selective and potent non-competitive mGlu5 antagonist (IC50 = 36 nM). Central effects following systemic administration in vivo.
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纯度
> 99% -
CAS编号
219911-35-0 -
化学结构
性能
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化学名称
2-Methyl-6-(phenylethynyl)pyridine hydrochloride -
分子量
229.71 -
分子式
C14H11N.HCl -
PubChem识别号
9794588 -
存放说明
Store at +4°C. Store under desiccating conditions. The product can be stored for up to 12 months. -
溶解度概述
Soluble in water to 5 mM, in ethanol to 100 mM and in DMSO to 100 mM -
处理
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 -
来源
Synthetic
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研究领域
图片
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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.
实验方案
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.
文献 (34)
ab120008 被引用在 34 文献中.
- Li YK et al. 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. J Neurosci Res 101:1170-1187 (2023). PubMed: 36807930
- Špirková A et al. Glutamate can act as a signaling molecule in mouse preimplantation embryos†. Biol Reprod 107:916-927 (2022). PubMed: 35746896
- Wong NF & Xu-Friedman MA Induction of Activity-Dependent Plasticity at Auditory Nerve Synapses. J Neurosci 42:6211-6220 (2022). PubMed: 35790402
- 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