MPEP hydrochloride

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1212/10
1212/50
MPEP hydrochloride | CAS No. 219911-35-0 | Group I mGluR Antagonists
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Description: Potent mGlu5 antagonist; also positive allosteric modulator of mGlu4 receptors

Chemical Name: 2-Methyl-6-(phenylethynyl)pyridine hydrochloride

Purity: ≥99%

Product Details
Citations (87)
Supplemental Products
Reviews (4)

Biological Activity

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.

Technical Data

M.Wt:
229.71
Formula:
C14H11N.HCl
Solubility:
Soluble to 5 mM in water with gentle warming and to 100 mM in DMSO
Purity:
≥99%
Storage:
Desiccate at +4°C
CAS No:
219911-35-0

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.

Background References

  1. Olanzapine: preclinical and clinical profiles of a novel antipsychotic agent.
    Tollefson and Taylor
    CNS Drug Reviews, 2000;6:303
  2. Antagonism of the mGlu5 agonist 2-chloro-5-hydroxyphenylglycine by the novel selective mGlu5 antagonist 6-methyl-2-(phenylethynyl)-pyridine (MPEP) in the thalamus.
    Salt et al.
    Br.J.Pharmacol., 1999;127:1057
  3. 2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist.
    Gasparini et al.
    Neuropharmacology, 1999;38:1493
  4. Positive allosteric modulation of the human metabotropic glutamate receptor 4 (hmGluR4) by SIB-1893 and MPEP.
    Mathiesen et al.
    Br.J.Pharmacol., 2003;138:1026
  5. Anti-hyperalgesic effects of the novel metabotropic glutamate receptor 5 antagonist, methylphenylethynylpyridine, in rat models of inflammatory pain.
    Bowes et al.
    Br.J.Pharmacol., 1999;126:250P

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Citations for MPEP hydrochloride

The citations listed below are publications that use Tocris products. Selected citations for MPEP hydrochloride include:

87 Citations: Showing 1 - 10

  1. Cortical layer 1 and layer 2/3 astrocytes exhibit distinct calcium dynamics in vivo.
    Authors: Takata and Hirase
    PLoS One  ;3:e2525
  2. Molecular components and functions of the endocannabinoid system in mouse prefrontal cortex.
    Authors: Lafourcade Et al.
    PLoS One  ;2:e709
  3. Synapse-specific opioid modulation of thalamo-cortico-striatal circuits.
    Authors: Birdsong Et al.
    Elife  2019;8
  4. A group I metabotropic glutamate receptor controls synaptic gain between rods and rod bipolar cells in the mouse retina.
    Authors: Hellmer Et al.
    Physiol Rep  2018;6:e13885
  5. DA Cells Differentially Regulate Striatal Cholinergic Transmission across Regions through Corelease of DA and Glutamate.
    Authors: Cai and Ford
    Cell Rep  2018;25:3148
  6. Astrocytic Activation Generates De Novo Neuronal Potentiation and Memory Enhancement.
    Authors: Adamsky Et al.
    Cell  2018;174:59
  7. Drebrin Isoforms Critically Regulate NMDAR- and mGluR-Dependent LTD Induction.
    Authors: Yasuda Et al.
    Front Cell Neurosci  2018;12:330
  8. LTP at Hilar Mossy Cell-Dentate Granule Cell Synapses Modulates Dentate Gyrus Output by Increasing Excitation/Inhibition Balance.
    Authors: Hashimotodani Et al.
    Neuron  2017;95:928
  9. The medullary dorsal reticular nucleus as a relay for descending pronociception induced by the mGluR5 in the rat infralimbic cortex.
    Authors: David-Pereira
    Neuroscience  2017;349:341
  10. Metabotropic glutamate receptor 5 mediates the suppressive effect of 6-OHDA-induced model of Parkinson's disease on liver cancer.
    Authors: Xi
    Pharmacol Res  2017;121:145
  11. Selective Disruption of Metabotropic Glutamate Receptor 5-Homer Interactions Mimics Phenotypes of Fragile X Syndrome in Mice.
    Authors: Guo Et al.
    J Neurosci  2016;36:2131
  12. Long-Term Potentiation at the Mossy Fiber-Granule Cell Relay Invokes Postsynaptic Second-Messenger Regulation of Kv4 Channels.
    Authors: Rizwan Et al.
    J Neurosci  2016;36:11196
  13. OE Facilitation of Cocaine Self-Administration in Female Rats Requires Activation of mGluR5.
    Authors: Martinez Et al.
    Eneuro  2016;3
  14. Mechanisms of tau and Aβ-induced excitotoxicity.
    Authors: Pallo Et al.
    Brain Res  2016;1634:119
  15. Acute inhibition of mGluR5 disrupts behavioral flexibility.
    Authors: Sethna and Wang
    Neurobiol Learn Mem  2016;130:1
  16. Multiple Drug Treatments That Increase cAMP Signaling Restore Long-Term Memory and Aberrant Signaling in Fragile X Syndrome Models.
    Authors: Choi Et al.
    Front Behav Neurosci  2016;10:136
  17. Augmentation of Ca(2+) signaling in astrocytic endfeet in the latent phase of temporal lobe epilepsy.
    Authors: Szokol Et al.
    Int J Mol Sci  2015;9:49
  18. The metabotropic glutamate receptor 5 role on motor behavior involves specific neural substrates.
    Authors: Guimaraes Et al.
    J Biol Chem  2015;8:24
  19. Relationship between in vivo receptor occupancy and efficacy of metabotropic glutamate receptor subtype 5 allosteric modulators with different in vitro binding profiles.
    Authors: Rook Et al.
    Clin Exp Dermatol  2015;40:755
  20. Abnormal excitability and episodic low-frequency oscillations in the cerebral cortex of the tottering mouse.
    Authors: Cramer Et al.
    PLoS One  2015;35:5664
  21. BDNF interacts with endocannabinoids to regulate cocaine-induced synaptic plasticity in mouse midbrain DA neurons.
    Authors: Zhong Et al.
    J Neurosci  2015;35:4469
  22. Homer protein-metabotropic glutamate receptor binding regulates endocannabinoid signaling and affects hyperexcitability in a mouse model of fragile X syndrome.
    Authors: Tang and Alger
    J Neurosci  2015;35:3938
  23. Synapse-specific compartmentalization of signaling cascades for LTP induction in CA3 interneurons.
    Authors: Galván Et al.
    Neuroscience  2015;290:332
  24. Nerve demyelination increases metabotropic glutamate receptor subtype 5 expression in peripheral painful mononeuropathy.
    Authors: Ko Et al.
    J Neurophysiol  2015;16:4642
  25. 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.
    Authors: Hullinger Et al.
    Neurobiol Learn Mem  2015;125:126
  26. Both neurons and astrocytes exhibited tetrodotoxin-resistant metabotropic glutamate receptor-dependent spontaneous slow Ca2+ oscillations in striatum.
    Authors: Tamura Et al.
    PLoS One  2014;9:e85351
  27. Hippocampal metaplasticity is required for the formation of temporal associative memories.
    Authors: Xu Et al.
    J Neurosci  2014;34:16762
  28. A novel mGluR5 antagonist, MFZ 10-7, inhibits cocaine-taking and cocaine-seeking behavior in rats.
    Authors: Keck Et al.
    Addict Biol  2014;19:195
  29. Effects of the mGluR5 antagonist MPEP on ethanol withdrawal induced anxiety-like syndrome in rats.
    Authors: Kumar Et al.
    Behav Brain Funct  2013;9:43
  30. The role of metabotropic glutamate receptor 5 on the stromal cell-derived factor-1/CXCR4 system in oral cancer.
    Authors: Kuribayashi Et al.
    Proc Natl Acad Sci U S A  2013;8:e80773
  31. Long lasting protein synthesis- and activity-dependent spine shrinkage and elimination after synaptic depression.
    Authors: Ramiro-Cortés and Israely
    PLoS One  2013;8:e71155
  32. NE drives persistent activity in prefrontal cortex via synergistic α1 and α2 adrenoceptors.
    Authors: Zhang Et al.
    PLoS One  2013;8:e66122
  33. Group II metabotropic glutamate receptors modify N-MthD.-aspartate receptors via Src kinase.
    Authors: Trepanier Et al.
    Sci Rep  2013;3:926
  34. NE enhances a discrete form of long-term depression during fear memory storage.
    Authors: Clem and Huganir
    J Neurosci  2013;33:11825
  35. Activation of mGluR5 and inhibition of NADPH oxidase improves functional recovery after traumatic brain injury.
    Authors: Loane Et al.
    J Neurosci  2013;30:403
  36. Synapse-specific and size-dependent mechanisms of spine structural plasticity accompanying synaptic weakening.
    Authors: Oh Et al.
    Proc Natl Acad Sci U S A  2013;110:E305
  37. Metabotropic glutamate receptor 5 within nucleus accumbens shell modulates environment-elicited cocaine conditioning expression.
    Authors: Martínez-Rivera Et al.
    Pharmacol Biochem Behav  2013;110:154
  38. Haploinsufficiency of Cyfip1 produces fragile X-like phenotypes in mice.
    Authors: Bozdagi Et al.
    J Neurosci  2012;7:e42422
  39. Metabotropic glutamate receptor 5 mediates phosphorylation of vascular endothelial cadherin and nuclear localization of β-catenin in response to homocysteine.
    Authors: Beard Et al.
    Vascul Pharmacol  2012;56:159
  40. Nitrative stress in cerebral endothelium is mediated by mGluR5 in hyperhomocysteinemia.
    Authors: Mayo Et al.
    J Cereb Blood Flow Metab  2012;32:825
  41. Endocannabinoid-mediated long-term depression of afferent excitatory synapses in hippocampal pyramidal cells and GABAergic interneurons.
    Authors: Peterfi Et al.
    J Neurosci  2012;32:14448
  42. Central amygdala metabotropic glutamate receptor 5 in the modulation of visceral pain.
    Authors: Crock Et al.
    J Neurotrauma  2012;32:14217
  43. Developmental regulation of CB1-mediated spike-time dependent depression at immature mossy fiber-CA3 synapses.
    Authors: Caiati Et al.
    Sci Rep  2012;2:285
  44. TRPV1-dependent and -independent alterations in the limbic cortex of neuropathic mice: impact on glial caspases and pain perception.
    Authors: Giordano Et al.
    Cereb Cortex  2012;22:2495
  45. Activity-dependent regulation of synaptic strength by PSD-95 in CA1 neurons.
    Authors: Zhang and Lisman
    J Neurosci  2012;107:1058
  46. Altered neocortical rhythmic activity states in Fmr1 KO mice are due to enhanced mGluR5 signaling and involve changes in excitatory circuitry.
    Authors: Hays Et al.
    J Neurosci  2011;31:14223
  47. Prolonged postinhibitory rebound firing in the cerebellar nuclei mediated by group I metabotropic glutamate receptor potentiation of L-type calcium currents.
    Authors: Zheng and Raman
    J Neurosci  2011;31:10283
  48. Interactive effects of mGlu5 and 5-HT2A receptors on locomotor activity in mice.
    Authors: Halberstadt Et al.
    Psychopharmacology (Berl)  2011;215:81
  49. An excitatory loop with astrocytes contributes to drive neurons to seizure threshold.
    Authors: Gómez-Gonzalo Et al.
    PLoS Biol  2010;8:e1000352
  50. Metabotropic glutamate receptor 5/Homer interactions underlie stress effects on fear.
    Authors: Tronson Et al.
    Front Cell Neurosci  2010;68:1007
  51. The maturation of GABAergic transmission in visual cortex requires endocannabinoid-mediated LTD of inhibitory inputs during a critical period.
    Authors: Jiang Et al.
    Neuron  2010;66:248
  52. Alterations in mGluR5 expression and signaling in Lewy body disease and in transgenic models of alpha-synucleinopathy--implications for excitotoxicity.
    Authors: Price Et al.
    PLoS One  2010;5:e14020
  53. Distinctions between persistent and reversible group I mGluR-induced epileptiform burst prolongation.
    Authors: Fuortes Et al.
    Epilepsia  2010;51:1633
  54. Sensory and cortical activation of distinct glial cell subtypes in the somatosensory thalamus of young rats.
    Authors: Parri Et al.
    Eur J Neurosci  2010;32:29
  55. Activation of metabotropic glutamate receptor 5 in the amygdala modulates pain-like behavior.
    Authors: Kolber Et al.
    PLoS One  2010;30:8203
  56. Discovery of a Novel Chemical Class of mGlu(5) Allosteric Ligands with Distinct Modes of Pharmacology.
    Authors: Hammond Et al.
    ACS Chem Neurosci  2010;1:702
  57. mGluR(1) Receptors Contribute to Non-Purinergic Slow Excitatory Transmission to Submucosal VIP Neurons of Guinea-Pig Ileum.
    Authors: Foong
    Front Neurosci  2009;3:46
  58. Modulator property of the intrinsic cortical projection from layer 6 to layer 4.
    Authors: Lee and Sherman
    Front Syst Neurosci  2009;3:3
  59. Non-Hebbian synaptic plasticity induced by repetitive postsynaptic action potentials.
    Authors: Kato Et al.
    J Neurosci  2009;29:11153
  60. Coupling of neural activity to blood flow in olfactory glomeruli is mediated by astrocytic pathways.
    Authors: Petzold Et al.
    Neuropharmacology  2008;58:897
  61. Dichotomous DArgic control of striatal synaptic plasticity.
    Authors: Shen Et al.
    Science  2008;321:848
  62. In vivo metabotropic glutamate receptor 5 (mGluR5) antagonism prevents cocaine-induced disruption of postsynaptically maintained mGluR5-dependent long-term depression.
    Authors: Grueter Et al.
    J Neurosci  2008;28:9261
  63. Roles of endocannabinoids in heterosynaptic long-term depression of excitatory synaptic transmission in visual cortex of young mice.
    Authors: Huang Et al.
    J Neurosci  2008;28:7074
  64. Group I metabotropic glutamate receptors control metaplasticity of spinal cord learning through a protein kinase C-dependent mechanism.
    Authors: Ferguson Et al.
    J Neurosci  2008;28:11939
  65. The tyrosine phosphatase STEP mediates AMPA receptor endocytosis after metabotropic glutamate receptor stimulation.
    Authors: Zhang Et al.
    J Neurosci  2008;28:10561
  66. Metabotropic glutamate receptor 1 (mGluR1) and 5 (mGluR5) regulate late phases of LTP and LTD in the hippocampal CA1 region in vitro.
    Authors: Neyman and Manahan-Vaughan
    Eur J Neurosci  2008;27:1345
  67. Aberrant early-phase ERK inactivation impedes neuronal function in fragile X syndrome.
    Authors: Kim Et al.
    J Neurosci  2008;105:4429
  68. AMPAR exocytosis through NO modulation of PICK1.
    Authors: Sossa Et al.
    Biol Psychiatry  2007;53:92
  69. Calpain-mediated mGluR1alpha truncation: a key step in excitotoxicity.
    Authors: Xu Et al.
    Neuron  2007;53:399
  70. Nonlinear regulation of unitary synaptic signals by CaV(2.3) voltage-sensitive calcium channels located in dendritic spines.
    Authors: Bloodgood and Sabatini
    Neuron  2007;53:249
  71. Loss of metabotropic glutamate receptor-dependent long-term depression via downregulation of mGluR5 after status epilepticus.
    Authors: Kirschstein Et al.
    J Neurosci  2007;27:7696
  72. Dysregulated metabotropic glutamate receptor-dependent translation of AMPA receptor and postsynaptic density-95 mRNAs at synapses in a mouse model of fragile X syndrome.
    Authors: Muddashetty Et al.
    J Neurosci  2007;27:5338
  73. Fragile X mental retardation protein deficiency leads to excessive mGluR5-dependent internalization of AMPA receptors.
    Authors: Nakamoto Et al.
    Proc Natl Acad Sci U S A  2007;104:15537
  74. Ionotropic and metabotropic glutamate receptor antagonism attenuates cue-induced cocaine seeking.
    Authors: Bäckström and Hyytiä
    Neuropsychopharmacology  2006;31:778
  75. Visual experience regulates metabotropic glutamate receptor-mediated plasticity of AMPA receptor synaptic transmission by homer1a induction.
    Authors: Keuren-Jensen and Cline
    J Neurosci  2006;26:7575
  76. Glutamatergic Control of Microvascular Tone by Distinct GABA Neurons in the Cerebellum.
    Authors: Rancillac Et al.
    Neuron  2006;26:6997
  77. Activation of group III metabotropic glutamate receptors attenuates rotenone toxicity on DArgic neurons through a microtubule-dependent mechanism.
    Authors: Jiang Et al.
    J Neurosci  2006;26:4318
  78. Stimulation of endocannabinoid formation in brain slice cultures through activation of group I metabotropic glutamate receptors.
    Authors: Jung Et al.
    Neuropsychopharmacology  2005;68:1196
  79. Phospholipase Cbeta serves as a coincidence detector through its Ca2+ dependency for triggering retrograde endocannabinoid signal.
    Authors: Hashimotodani Et al.
    Neuron  2005;45:257
  80. Functional metabotropic glutamate receptors on nuclei from brain and primary cultured striatal neurons. Role of transporters in delivering ligand.
    Authors: Jong Et al.
    Mol Pharmacol  2005;280:30469
  81. Interactions between ephrin-B and metabotropic glutamate 1 receptors in brain tissue and cultured neurons.
    Authors: Calò Et al.
    J Neurosci  2005;25:2245
  82. Group I metabotropic glutamate receptor activation produces a direct excitation of identified septohippocampal cholinergic neurons.
    Authors: Wu Et al.
    J Neurophysiol  2004;92:1216
  83. Endocannabinoid-mediated metaplasticity in the hippocampus.
    Authors: Chevaleyre and Castillo
    Neuron  2004;43:871
  84. Extracellular signal-regulated protein kinase activation is required for metabotropic glutamate receptor-dependent long-term depression in hippocampal area CA1.
    Authors: Gallagher Et al.
    Mol Brain  2004;24:4859
  85. Prefrontal cortex stimulation induces 2-arachidonoyl-glycerol-mediated suppression of excitation in DA neurons.
    Authors: Melis Et al.
    J Neurosci  2004;24:10707
  86. Positive allosteric modulation of the human metabotropic glutamate receptor 4 (hmGluR4) by SIB-1893 and MPEP.
    Authors: Mathiesen Et al.
    Br J Pharmacol  2003;138:1026
  87. Metabotropic mGlu5 receptors regulate adenosine A2A receptor signaling.
    Authors: Nishi Et al.
    J Neurosci  2003;100:1322

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Used in inhibitor cocktail
By Anonymous on 12/03/2019
Application: Species: Rat

Retinal dissections were performed in HEPES-buffered extracellular solution containing glutamate inhibitor cocktail with 50 umol/L MPEP

PMID: 30338673

mGluR5 antagonist (10 µM)
By Kang Peng on 09/18/2018
Application: Species: Mouse

mGluR5 antagonist (10 µM)


mGluR5 antagonist
By Kang Peng on 06/05/2018
Application: Species: Mouse

We use MPEP Hydrochloride as the mGluR5 antagonist in 10 uM.


Succesfull block of mGluRs
By Anonymous on 11/02/2017
Application: Species: Rat

We use bath application of CPCCOEt and MPEP to block mGluRs.


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