MPEP,mGlu 5拮抗剂

货号 (SKU)	包装规格	是否现货
M127959-10mg	10mg	现货
M127959-50mg	50mg	现货
M127959-250mg	250mg	现货
M127959-1g	1g	现货

基本描述

别名	2-甲基-6-(苯基乙炔基)吡啶
英文别名	MPEP\|2-Methyl-6-(phenylethynyl)pyridine\|96206-92-7\|6-Methyl-2-(phenylethynyl)pyridine\|2-methyl-6-(2-phenylethynyl)pyridine\|7VC0YVI27Y\|CHEMBL66654\|CHEBI:64159\|Pyridine, 2-methyl-6-(phenylethynyl)-\|2-methyl-6-(phenylethynyl)-pyridine\|Tocris-1212\|Lopac-M-543
规格或纯度	≥98%
英文名称	MPEP
生化机理	MPEP is a potent and highly selective non-competitive antagonist at the mGlu5 receptor subtype (IC50 = 36 nM) and a positive allosteric modulator at mGlu4 receptors. Centrally active following systemic administration in vivo. Reverses mechanical hyperalgesia in the inflamed rat hind paw.Subtype selective and potent non-competitive mGlu 5 antagonist (IC 50 = 36 nM). Central effects following systemic administration in vivo .
储存温度	-20°C储存,充氩
运输条件	超低温冰袋运输
备注	如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，它们最多可以使用一个月。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。
产品介绍	MPEP是mGlu5受体非竞争性拮抗剂，IC50为36 nM，还是mGlu4受体的正向变构调节剂。 MPEP is a selective mGlu5 receptor antagonist with IC50 of 36 nM, exhibits no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors.

名称和标识符

PubChem SID	488194193
IUPAC Name	2-methyl-6-(2-phenylethynyl)pyridine
INCHI	InChI=1S/C14H11N/c1-12-6-5-9-14(15-12)11-10-13-7-3-2-4-8-13/h2-9H,1H3
InChi Key	NEWKHUASLBMWRE-UHFFFAOYSA-N
Canonical SMILES	CC1=NC(=CC=C1)C#CC2=CC=CC=C2
Isomeric SMILES	CC1=NC(=CC=C1)C#CC2=CC=CC=C2
PubChem CID	3025961
分子量	193.24

数据库链接

PubChem CID	3025961
Wikipedia	2-Methyl-6-(phenylethynyl)pyridine
ChEMBL Ligand	CHEMBL66654
BindingDB Ligand	50084137
CAS Registry No.	96206-92-7
GPCRdb Ligand	MPEP
PubChem SID	488194193

化学和物理性质

溶解性	DMSO 39 mg/mL Water <1 mg/mL Ethanol 39 mg/mL
敏感性	对空气敏感；对热敏感
熔点	47 °C

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参考文献

1. Dickinson BA et al.. (2009) A novel mechanism of hippocampal LTD involving muscarinic receptor-triggered interactions between AMPARs, GRIP and liprin-alpha.. Mol Brain, 2 (): (18). [PMID:19534762]
2. Gómez-Gonzalo M et al.. (2010) An excitatory loop with astrocytes contributes to drive neurons to seizure threshold.. PLoS Biol, 8 (4): (e1000352). [PMID:20405049]
3. Min R & Nevian T. (2012) Astrocyte signaling controls spike timing-dependent depression at neocortical synapses.. Nat Neurosci, 15 (5): (746-53). [PMID:22446881]
4. Younts TJ et al.. (2013) CA1 pyramidal cell theta-burst firing triggers endocannabinoid-mediated long-term depression at both somatic and dendritic inhibitory synapses.. J Neurosci, 33 (34): (13743-57). [PMID:23966696]
5. Droste D et al.. (2017) Ca2+-permeable AMPA receptors in mouse olfactory bulb astrocytes.. Sci Rep, 7 (): (44817). [PMID:28322255]
6. Ran I et al.. (2012) CREB-dependent transcriptional control and quantal changes in persistent long-term potentiation in hippocampal interneurons.. J Neurosci, 32 (18): (6335-50). [PMID:22553039]
7. Shin JH et al.. (2009) Depolarization-induced slow current in cerebellar Purkinje cells does not require metabotropic glutamate receptor 1.. Neuroscience, 162 (3): (688-93). [PMID:19409231]
8. Yang Y & Xu-Friedman MA. (2015) Different pools of glutamate receptors mediate sensitivity to ambient glutamate in the cochlear nucleus.. J Neurophysiol, 113 (10): (3634-45). [PMID:25855696]
9. Bragina L et al.. (2015) Differential expression of metabotropic glutamate and GABA receptors at neocortical glutamatergic and GABAergic axon terminals.. Front Cell Neurosci, 9 (): (345). [PMID:26388733]
10. Nasrallah C et al.. (2018) Direct coupling of detergent purified human mGlu5 receptor to the heterotrimeric G proteins Gq and Gs.. Sci Rep, 8 (): (4407). [PMID:29535347]
11. Krishnan B et al.. (2011) Dopamine-induced plasticity, phospholipase D (PLD) activity and cocaine-cue behavior depend on PLD-linked metabotropic glutamate receptors in amygdala.. PLoS One, 6 (9): (e25639). [PMID:21980514]
12. Chiu CQ et al.. (2010) Dopaminergic modulation of endocannabinoid-mediated plasticity at GABAergic synapses in the prefrontal cortex.. J Neurosci, 30 (21): (7236-48). [PMID:20505090]
13. Andlauer TF et al.. (2014) Drep-2 is a novel synaptic protein important for learning and memory.. Elife, 3 (): (). [PMID:25392983]
14. Ster J et al.. (2011) Enhancement of CA3 hippocampal network activity by activation of group II metabotropic glutamate receptors.. Proc Natl Acad Sci U S A, 108 (24): (9993-7). [PMID:21628565]
15. Li Y et al.. (2012) Epileptic stimulus increases Homer 1a expression to modulate endocannabinoid signaling in cultured hippocampal neurons.. Neuropharmacology, 63 (6): (1140-9). [PMID:22814532]
16. Li Y et al.. (2013) Epileptiform stimulus increases Homer 1a expression to modulate synapse number and activity in hippocampal cultures.. J Neurophysiol, 109 (6): (1494-504). [PMID:23274309]
17. Chanda S & Xu-Friedman MA. (2011) Excitatory modulation in the cochlear nucleus through group I metabotropic glutamate receptor activation.. J Neurosci, 31 (20): (7450-5). [PMID:21593328]
18. Špirková A et al.. (2022) Glutamate can act as a signaling molecule in mouse preimplantation embryos†.. Biol Reprod, 107 (4): (916-927). [PMID:35746896]
19. Li DP & Pan HL. (2010) Increased group I metabotropic glutamate receptor activity in paraventricular nucleus supports elevated sympathetic vasomotor tone in hypertension.. Am J Physiol Regul Integr Comp Physiol, 299 (2): (R552-61). [PMID:20519363]
20. Colavita M et al.. (2016) Layer-specific potentiation of network GABAergic inhibition in the CA1 area of the hippocampus.. Sci Rep, 6 (): (28454). [PMID:27345695]
21. Liu MG et al.. (2013) Long-term potentiation of synaptic transmission in the adult mouse insular cortex: multielectrode array recordings.. J Neurophysiol, 110 (2): (505-21). [PMID:23636718]
22. Mares P et al.. (2010) Metabotropic glutamate receptors as a target for anticonvulsant and anxiolytic action in immature rats.. Epilepsia, 51 Suppl 3 (): (24-6). [PMID:20618395]
23. Jo J et al.. (2010) Muscarinic receptors induce LTD of NMDAR EPSCs via a mechanism involving hippocalcin, AP2 and PSD-95.. Nat Neurosci, 13 (10): (1216-24). [PMID:20852624]
24. Ledonne A et al.. (2014) Neuregulin 1 signalling modulates mGluR1 function in mesencephalic dopaminergic neurons.. Mol Psychiatry, (): (). [PMID:25266126]
25. Molina-Obando S et al.. (2019) ON selectivity in the Drosophila visual system is a multisynaptic process involving both glutamatergic and GABAergic inhibition.. Elife, 8 (): (). [PMID:31535971]
26. Ran I et al.. (2009) Persistent transcription- and translation-dependent long-term potentiation induced by mGluR1 in hippocampal interneurons.. J Neurosci, 29 (17): (5605-15). [PMID:19403827]
27. Habbas S et al.. (2011) Purinergic signaling in the cerebellum: Bergmann glial cells express functional ionotropic P2X7 receptors.. Glia, 59 (12): (1800-12). [PMID:21830236]
28. Li JQ et al.. (2010) Regulation of increased glutamatergic input to spinal dorsal horn neurons by mGluR5 in diabetic neuropathic pain.. J Neurochem, 112 (): (162-72). [PMID:19840219]
29. Latif-Hernandez A et al.. (2016) 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). [PMID:27872582]
30. Qi Y et al.. (2012) Switching off LTP: mGlu and NMDA Receptor-Dependent Novelty Exploration-Induced Depotentiation in the Rat Hippocampus.. Cereb Cortex, (): (). [PMID:22490551]
31. Brown JT et al.. (2011) Synaptic activation of mGluR1 generates persistent depression of a fast after-depolarizing potential in CA3 pyramidal neurons.. Eur J Neurosci, 33 (5): (879-89). [PMID:21269340]

MPEP,mGlu 5拮抗剂

库存信息

库存信息

库存信息

库存信息

基本描述

名称和标识符

数据库链接

化学和物理性质

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