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Biological Activity for MPEP hydrochloride
MPEP hydrochloride 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.
Compound Libraries for MPEP hydrochloride
Technical Data for MPEP hydrochloride
|Storage||Desiccate at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for MPEP hydrochloride
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|water||1.15||5 with gentle warming|
Preparing Stock Solutions for MPEP hydrochloride
The following data is based on the product molecular weight 229.71. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||4.35 mL||21.77 mL||43.53 mL|
|5 mM||0.87 mL||4.35 mL||8.71 mL|
|10 mM||0.44 mL||2.18 mL||4.35 mL|
|50 mM||0.09 mL||0.44 mL||0.87 mL|
Product Datasheets for MPEP hydrochloride
References for MPEP hydrochloride
References are publications that support the biological activity of the product.
Gasparini et al (1999) 2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist. Neuropharmacology 38 1493 PMID: 10530811
Mathiesen et al (2003) Positive allosteric modulation of the human metabotropic glutamate receptor 4 (hmGluR4) by SIB-1893 and MPEP. Br.J.Pharmacol. 138 1026 PMID: 12684257
Salt et al (1999) Antagonism of the mGlu5 agonist 2-chloro-5-hydroxyphenylglycine by the novel selective mGlu5 antagonist 6-methyl-2-(phenylethynyl)-pyridine (MPEP) in the thalamus. Br.J.Pharmacol. 127 1057 PMID: 10455248
Bowes et al (1999) Anti-hyperalgesic effects of the novel metabotropic glutamate receptor 5 antagonist, methylphenylethynylpyridine, in rat models of inflammatory pain. Br.J.Pharmacol. 126 250P
If you know of a relevant reference for MPEP hydrochloride, please let us know.
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Keywords: MPEP hydrochloride, MPEP hydrochloride supplier, mGlu5, mGluR5, antagonists, positive, allosteric, modulators, mGlu4, mGluR4, PAM, Positive, Group, I, Receptors, Glutamate, Metabotropic, III, (Metabotropic), 1212, Tocris Bioscience
87 Citations for MPEP hydrochloride
Citations are publications that use Tocris products. Selected citations for MPEP hydrochloride include:
Tang and Alger (2015) Homer protein-metabotropic glutamate receptor binding regulates endocannabinoid signaling and affects hyperexcitability in a mouse model of fragile X syndrome. J Neurosci 35 3938 PMID: 25740522
Tamura et al (2014) Both neurons and astrocytes exhibited tetrodotoxin-resistant metabotropic glutamate receptor-dependent spontaneous slow Ca2+ oscillations in striatum. PLoS One 9 e85351 PMID: 24454845
Loane et al (2013) Activation of mGluR5 and inhibition of NADPH oxidase improves functional recovery after traumatic brain injury. J Neurosci 30 403 PMID: 23199080
Kuribayashi et al (2013) The role of metabotropic glutamate receptor 5 on the stromal cell-derived factor-1/CXCR4 system in oral cancer. Proc Natl Acad Sci U S A 8 e80773 PMID: 24236200
Halberstadt et al (2011) Interactive effects of mGlu5 and 5-HT2A receptors on locomotor activity in mice. Psychopharmacology (Berl) 215 81 PMID: 21153406
Hays et al (2011) Altered neocortical rhythmic activity states in Fmr1 KO mice are due to enhanced mGluR5 signaling and involve changes in excitatory circuitry. J Neurosci 31 14223 PMID: 21976507
Shen et al (2008) Dichotomous DArgic control of striatal synaptic plasticity. Science 321 848 PMID: 18687967
Zhang et al (2008) The tyrosine phosphatase STEP mediates AMPA receptor endocytosis after metabotropic glutamate receptor stimulation. J Neurosci 28 10561 PMID: 18923032
Neyman and Manahan-Vaughan (2008) Metabotropic glutamate receptor 1 (mGluR1) and 5 (mGluR5) regulate late phases of LTP and LTD in the hippocampal CA1 region in vitro. Eur J Neurosci 27 1345 PMID: 18364018
Ferguson et al (2008) Group I metabotropic glutamate receptors control metaplasticity of spinal cord learning through a protein kinase C-dependent mechanism. J Neurosci 28 11939 PMID: 19005059
Grueter et al (2008) In vivo metabotropic glutamate receptor 5 (mGluR5) antagonism prevents cocaine-induced disruption of postsynaptically maintained mGluR5-dependent long-term depression. J Neurosci 28 9261 PMID: 18784306
Birdsong et al (2019) Synapse-specific opioid modulation of thalamo-cortico-striatal circuits. Elife 8 PMID: 31099753
Sethna and Wang (2016) Acute inhibition of mGluR5 disrupts behavioral flexibility. Neurobiol Learn Mem 130 1 PMID: 26777993
Pallo et al (2016) Mechanisms of tau and Aβ-induced excitotoxicity. Brain Res 1634 119 PMID: 26731336
Bozdagi et al (2012) Haploinsufficiency of Cyfip1 produces fragile X-like phenotypes in mice. J Neurosci 7 e42422 PMID: 22900020
Crock et al (2012) Central amygdala metabotropic glutamate receptor 5 in the modulation of visceral pain. J Neurotrauma 32 14217 PMID: 23055491
Huang et al (2008) Roles of endocannabinoids in heterosynaptic long-term depression of excitatory synaptic transmission in visual cortex of young mice. J Neurosci 28 7074 PMID: 18614676
Bloodgood and Sabatini (2007) Nonlinear regulation of unitary synaptic signals by CaV(2.3) voltage-sensitive calcium channels located in dendritic spines. Neuron 53 249 PMID: 17224406
Kirschstein et al (2007) Loss of metabotropic glutamate receptor-dependent long-term depression via downregulation of mGluR5 after status epilepticus. J Neurosci 27 7696 PMID: 17634364
Xu et al (2007) Calpain-mediated mGluR1alpha truncation: a key step in excitotoxicity. Neuron 53 399 PMID: 17270736
Muddashetty et al (2007) Dysregulated metabotropic glutamate receptor-dependent translation of AMPA receptor and postsynaptic density-95 mRNAs at synapses in a mouse model of fragile X syndrome. J Neurosci 27 5338 PMID: 17507556
Nakamoto et al (2007) Fragile X mental retardation protein deficiency leads to excessive mGluR5-dependent internalization of AMPA receptors. Proc Natl Acad Sci U S A 104 15537 PMID: 17881561
Cai and Ford (2018) DA Cells Differentially Regulate Striatal Cholinergic Transmission across Regions through Corelease of DA and Glutamate. Cell Rep 25 3148 PMID: 30540946
Xu et al (2014) Hippocampal metaplasticity is required for the formation of temporal associative memories. J Neurosci 34 16762 PMID: 25505329
Keck et al (2014) A novel mGluR5 antagonist, MFZ 10-7, inhibits cocaine-taking and cocaine-seeking behavior in rats. Addict Biol 19 195 PMID: 24001208
Tronson et al (2010) Metabotropic glutamate receptor 5/Homer interactions underlie stress effects on fear. Front Cell Neurosci 68 1007 PMID: 21075228
Kolber et al (2010) Activation of metabotropic glutamate receptor 5 in the amygdala modulates pain-like behavior. PLoS One 30 8203 PMID: 20554871
Sossa et al (2007) AMPAR exocytosis through NO modulation of PICK1. Biol Psychiatry 53 92 PMID: 17555774
Rancillac et al (2006) Glutamatergic Control of Microvascular Tone by Distinct GABA Neurons in the Cerebellum. Neuron 26 6997 PMID: 16807329
Adamsky et al (2018) Astrocytic Activation Generates De Novo Neuronal Potentiation and Memory Enhancement. Cell 174 59 PMID: 29804835
Guo et al (2016) Selective Disruption of Metabotropic Glutamate Receptor 5-Homer Interactions Mimics Phenotypes of Fragile X Syndrome in Mice. J Neurosci 36 2131 PMID: 26888925
Martinez et al (2016) OE Facilitation of Cocaine Self-Administration in Female Rats Requires Activation of mGluR5. Eneuro 3 PMID: 27822496
Rook et al (2015) Relationship between in vivo receptor occupancy and efficacy of metabotropic glutamate receptor subtype 5 allosteric modulators with different in vitro binding profiles. Clin Exp Dermatol 40 755 PMID: 25241804
Szokol et al (2015) Augmentation of Ca(2+) signaling in astrocytic endfeet in the latent phase of temporal lobe epilepsy. Int J Mol Sci 9 49 PMID: 25762896
Ko et al (2015) Nerve demyelination increases metabotropic glutamate receptor subtype 5 expression in peripheral painful mononeuropathy. J Neurophysiol 16 4642 PMID: 25739080
Zhong et al (2015) BDNF interacts with endocannabinoids to regulate cocaine-induced synaptic plasticity in mouse midbrain DA neurons. J Neurosci 35 4469 PMID: 25762688
Cramer et al (2015) Abnormal excitability and episodic low-frequency oscillations in the cerebral cortex of the tottering mouse. PLoS One 35 5664 PMID: 25855180
Guimaraes et al (2015) The metabotropic glutamate receptor 5 role on motor behavior involves specific neural substrates. J Biol Chem 8 24 PMID: 25885370
Mayo et al (2012) Nitrative stress in cerebral endothelium is mediated by mGluR5 in hyperhomocysteinemia. J Cereb Blood Flow Metab 32 825 PMID: 22186670
Caiati et al (2012) Developmental regulation of CB1-mediated spike-time dependent depression at immature mossy fiber-CA3 synapses. Sci Rep 2 285 PMID: 22368777
Price et al (2010) Alterations in mGluR5 expression and signaling in Lewy body disease and in transgenic models of alpha-synucleinopathy--implications for excitotoxicity. PLoS One 5 e14020 PMID: 21103359
Jiang et al (2010) The maturation of GABAergic transmission in visual cortex requires endocannabinoid-mediated LTD of inhibitory inputs during a critical period. Neuron 66 248 PMID: 20435001
Gómez-Gonzalo et al (2010) An excitatory loop with astrocytes contributes to drive neurons to seizure threshold. PLoS Biol 8 e1000352 PMID: 20405049
Hammond et al (2010) Discovery of a Novel Chemical Class of mGlu(5) Allosteric Ligands with Distinct Modes of Pharmacology. ACS Chem Neurosci 1 702 PMID: 20981342
Fuortes et al (2010) Distinctions between persistent and reversible group I mGluR-induced epileptiform burst prolongation. Epilepsia 51 1633 PMID: 20659148
Parri et al (2010) Sensory and cortical activation of distinct glial cell subtypes in the somatosensory thalamus of young rats. Eur J Neurosci 32 29 PMID: 20608967
Bäckström and Hyytiä (2006) Ionotropic and metabotropic glutamate receptor antagonism attenuates cue-induced cocaine seeking. Neuropsychopharmacology 31 778 PMID: 16123768
Keuren-Jensen and Cline (2006) Visual experience regulates metabotropic glutamate receptor-mediated plasticity of AMPA receptor synaptic transmission by homer1a induction. J Neurosci 26 7575 PMID: 16855085
Jiang et al (2006) Activation of group III metabotropic glutamate receptors attenuates rotenone toxicity on DArgic neurons through a microtubule-dependent mechanism. J Neurosci 26 4318 PMID: 16624952
Hashimotodani et al (2005) Phospholipase Cbeta serves as a coincidence detector through its Ca2+ dependency for triggering retrograde endocannabinoid signal. Neuron 45 257 PMID: 15664177
David-Pereira (2017) The medullary dorsal reticular nucleus as a relay for descending pronociception induced by the mGluR5 in the rat infralimbic cortex. Neuroscience 349 341 PMID: 28300633
Xi (2017) Metabotropic glutamate receptor 5 mediates the suppressive effect of 6-OHDA-induced model of Parkinson's disease on liver cancer. Pharmacol Res 121 145 PMID: 28455267
Giordano et al (2012) TRPV1-dependent and -independent alterations in the limbic cortex of neuropathic mice: impact on glial caspases and pain perception. Cereb Cortex 22 2495 PMID: 22139792
Kato et al (2009) Non-Hebbian synaptic plasticity induced by repetitive postsynaptic action potentials. J Neurosci 29 11153 PMID: 19741122
Foong (2009) mGluR(1) Receptors Contribute to Non-Purinergic Slow Excitatory Transmission to Submucosal VIP Neurons of Guinea-Pig Ileum. Front Neurosci 3 46 PMID: 20582273
Chevaleyre and Castillo (2004) Endocannabinoid-mediated metaplasticity in the hippocampus. Neuron 43 871 PMID: 15363397
Melis et al (2004) Prefrontal cortex stimulation induces 2-arachidonoyl-glycerol-mediated suppression of excitation in DA neurons. J Neurosci 24 10707 PMID: 15564588
Wu et al (2004) Group I metabotropic glutamate receptor activation produces a direct excitation of identified septohippocampal cholinergic neurons. J Neurophysiol 92 1216 PMID: 15044519
Mathiesen et al (2003) Positive allosteric modulation of the human metabotropic glutamate receptor 4 (hmGluR4) by SIB-1893 and MPEP. Br J Pharmacol 138 1026 PMID: 12684257
Nishi et al (2003) Metabotropic mGlu5 receptors regulate adenosine A2A receptor signaling. J Neurosci 100 1322 PMID: 12538871
Hashimotodani et al (2017) LTP at Hilar Mossy Cell-Dentate Granule Cell Synapses Modulates Dentate Gyrus Output by Increasing Excitation/Inhibition Balance. Neuron 95 928 PMID: 28817805
Hullinger et al (2015) Environmental enrichment improves learning and memory and long-term potentiation in young adult rats through a mechanism requiring mGluR5 signaling and sustained activation of p70s6k. Neurobiol Learn Mem 125 126 PMID: 26341144
Galván et al (2015) Synapse-specific compartmentalization of signaling cascades for LTP induction in CA3 interneurons. Neuroscience 290 332 PMID: 25637803
Trepanier et al (2013) Group II metabotropic glutamate receptors modify N-MthD.-aspartate receptors via Src kinase. Sci Rep 3 926 PMID: 23378895
Kumar et al (2013) Effects of the mGluR5 antagonist MPEP on ethanol withdrawal induced anxiety-like syndrome in rats. Behav Brain Funct 9 43 PMID: 24279870
Ramiro-Cortés and Israely (2013) Long lasting protein synthesis- and activity-dependent spine shrinkage and elimination after synaptic depression. PLoS One 8 e71155 PMID: 23951097
Zheng and Raman (2011) Prolonged postinhibitory rebound firing in the cerebellar nuclei mediated by group I metabotropic glutamate receptor potentiation of L-type calcium currents. J Neurosci 31 10283 PMID: 21753005
Lee and Sherman (2009) Modulator property of the intrinsic cortical projection from layer 6 to layer 4. Front Syst Neurosci 3 3 PMID: 19277215
Takata and Hirase Cortical layer 1 and layer 2/3 astrocytes exhibit distinct calcium dynamics in vivo. PLoS One 3 e2525 PMID: 18575586
Lafourcade et al Molecular components and functions of the endocannabinoid system in mouse prefrontal cortex. PLoS One 2 e709 PMID: 17684555
Hellmer et al (2018) A group I metabotropic glutamate receptor controls synaptic gain between rods and rod bipolar cells in the mouse retina. Physiol Rep 6 e13885 PMID: 30338673
Yasuda et al (2018) Drebrin Isoforms Critically Regulate NMDAR- and mGluR-Dependent LTD Induction. Front Cell Neurosci 12 330 PMID: 30349460
Kim et al (2008) Aberrant early-phase ERK inactivation impedes neuronal function in fragile X syndrome. J Neurosci 105 4429 PMID: 18332424
Petzold et al (2008) Coupling of neural activity to blood flow in olfactory glomeruli is mediated by astrocytic pathways. Neuropharmacology 58 897 PMID: 18579080
Rizwan et al (2016) Long-Term Potentiation at the Mossy Fiber-Granule Cell Relay Invokes Postsynaptic Second-Messenger Regulation of Kv4 Channels. J Neurosci 36 11196 PMID: 27807163
Choi et al (2016) Multiple Drug Treatments That Increase cAMP Signaling Restore Long-Term Memory and Aberrant Signaling in Fragile X Syndrome Models. Front Behav Neurosci 10 136 PMID: 27445731
Martínez-Rivera et al (2013) Metabotropic glutamate receptor 5 within nucleus accumbens shell modulates environment-elicited cocaine conditioning expression. Pharmacol Biochem Behav 110 154 PMID: 23850523
Clem and Huganir (2013) NE enhances a discrete form of long-term depression during fear memory storage. J Neurosci 33 11825 PMID: 23864672
Zhang et al (2013) NE drives persistent activity in prefrontal cortex via synergistic α1 and α2 adrenoceptors. PLoS One 8 e66122 PMID: 23785477
Oh et al (2013) Synapse-specific and size-dependent mechanisms of spine structural plasticity accompanying synaptic weakening. Proc Natl Acad Sci U S A 110 E305 PMID: 23269840
Zhang and Lisman (2012) Activity-dependent regulation of synaptic strength by PSD-95 in CA1 neurons. J Neurosci 107 1058 PMID: 22114157
Peterfi et al (2012) Endocannabinoid-mediated long-term depression of afferent excitatory synapses in hippocampal pyramidal cells and GABAergic interneurons. J Neurosci 32 14448 PMID: 23055515
Beard et al (2012) Metabotropic glutamate receptor 5 mediates phosphorylation of vascular endothelial cadherin and nuclear localization of β-catenin in response to homocysteine. Vascul Pharmacol 56 159 PMID: 22285407
Calò et al (2005) Interactions between ephrin-B and metabotropic glutamate 1 receptors in brain tissue and cultured neurons. J Neurosci 25 2245 PMID: 15745950
Jong et al (2005) Functional metabotropic glutamate receptors on nuclei from brain and primary cultured striatal neurons. Role of transporters in delivering ligand. Mol Pharmacol 280 30469 PMID: 15958386
Jung et al (2005) Stimulation of endocannabinoid formation in brain slice cultures through activation of group I metabotropic glutamate receptors. Neuropsychopharmacology 68 1196 PMID: 16051747
Gallagher et al (2004) Extracellular signal-regulated protein kinase activation is required for metabotropic glutamate receptor-dependent long-term depression in hippocampal area CA1. Mol Brain 24 4859 PMID: 15152046
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Retinal dissections were performed in HEPES-buffered extracellular solution containing glutamate inhibitor cocktail with 50 umol/L MPEP
mGluR5 antagonist (10 µM)
We use MPEP Hydrochloride as the mGluR5 antagonist in 10 uM.
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.
Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.
Huntington's Disease Poster
Huntington's disease (HD) is a monogenic neurodegenerative disorder, which is characterized by the prevalent loss of GABAergic medium spiny neurons (MSN) in the striatum. This poster summarizes the MSN intracellular signaling pathways implicated in the pathology of HD, as well as highlighting the use of iPSCs for HD modeling.
Learning & Memory Poster
Recognition memory enables us to make judgements about whether or not we have encountered a particular stimulus before. This poster outlines the cellular mechanisms underlying recognition memory and its links to long-term depression, as well as the use of pharmacological intervention to assess the role of neurotransmitters in recognition memory.
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Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.