MPEP hydrochloride

  ( 73 citations ) ( 1 Review )    
Product Datasheet
Catalog Number:1212
Chemical Name:2-Methyl-6-(phenylethynyl)pyridine hydrochloride
Product Details
Citations (73)
Supplemental Products
Reviews
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. Also available as part of the Group I mGlu Receptor Tocriset™.
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. All Tocris products are intended for laboratory research use only.
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Citations:

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

73 Citations: Showing 1 - 10
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  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. 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
  4. 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
  5. 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
  6. Estradiol Facilitation of Cocaine Self-Administration in Female Rats Requires Activation of mGluR5.
    Authors: Martinez Et al.
    Eneuro  2016;3
  7. 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
  8. The metabotropic glutamate receptor 5 role on motor behavior involves specific neural substrates.
    Authors: Guimaraes Et al.
    J Biol Chem  2015;8:24
  9. 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
  10. Abnormal excitability and episodic low-frequency oscillations in the cerebral cortex of the tottering mouse.
    Authors: Cramer Et al.
    PLoS One  2015;35:5664
  11. BDNF interacts with endocannabinoids to regulate cocaine-induced synaptic plasticity in mouse midbrain dopamine neurons.
    Authors: Zhong Et al.
    J Neurosci  2015;35:4469
  12. 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
  13. Synapse-specific compartmentalization of signaling cascades for LTP induction in CA3 interneurons.
    Authors: Galván Et al.
    Neuroscience  2015;290:332
  14. Nerve demyelination increases metabotropic glutamate receptor subtype 5 expression in peripheral painful mononeuropathy.
    Authors: Ko Et al.
    J Neurophysiol  2015;16:4642
  15. 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
  16. 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
  17. Hippocampal metaplasticity is required for the formation of temporal associative memories.
    Authors: Xu Et al.
    J Neurosci  2014;34:16762
  18. 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
  19. 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
  20. 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
  21. Long lasting protein synthesis- and activity-dependent spine shrinkage and elimination after synaptic depression.
    Authors: Ramiro-Cortés and Israely
    PLoS One  2013;8:e71155
  22. Norepinephrine drives persistent activity in prefrontal cortex via synergistic α1 and α2 adrenoceptors.
    Authors: Zhang Et al.
    PLoS One  2013;8:e66122
  23. Group II metabotropic glutamate receptors modify N-methyl-D-aspartate receptors via Src kinase.
    Authors: Trepanier Et al.
    Sci Rep  2013;3:926
  24. Norepinephrine enhances a discrete form of long-term depression during fear memory storage.
    Authors: Clem and Huganir
    J Neurosci  2013;33:11825
  25. Activation of mGluR5 and inhibition of NADPH oxidase improves functional recovery after traumatic brain injury.
    Authors: Loane Et al.
    J Neurosci  2013;30:403
  26. 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
  27. 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
  28. Haploinsufficiency of Cyfip1 produces fragile X-like phenotypes in mice.
    Authors: Bozdagi Et al.
    J Neurosci  2012;7:e42422
  29. 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
  30. Nitrative stress in cerebral endothelium is mediated by mGluR5 in hyperhomocysteinemia.
    Authors: Mayo Et al.
    J Cereb Blood Flow Metab  2012;32:825
  31. 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
  32. Central amygdala metabotropic glutamate receptor 5 in the modulation of visceral pain.
    Authors: Crock Et al.
    J Neurotrauma  2012;32:14217
  33. Developmental regulation of CB1-mediated spike-time dependent depression at immature mossy fiber-CA3 synapses.
    Authors: Caiati Et al.
    Sci Rep  2012;2:285
  34. 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
  35. Activity-dependent regulation of synaptic strength by PSD-95 in CA1 neurons.
    Authors: Zhang and Lisman
    J Neurosci  2012;107:1058
  36. 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
  37. 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
  38. Interactive effects of mGlu5 and 5-HT2A receptors on locomotor activity in mice.
    Authors: Halberstadt Et al.
    Psychopharmacology (Berl)  2011;215:81
  39. An excitatory loop with astrocytes contributes to drive neurons to seizure threshold.
    Authors: Gómez-Gonzalo Et al.
    PLoS Biol  2010;8:e1000352
  40. Metabotropic glutamate receptor 5/Homer interactions underlie stress effects on fear.
    Authors: Tronson Et al.
    Front Cell Neurosci  2010;68:1007
  41. 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
  42. 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
  43. Distinctions between persistent and reversible group I mGluR-induced epileptiform burst prolongation.
    Authors: Fuortes Et al.
    Epilepsia  2010;51:1633
  44. 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
  45. Activation of metabotropic glutamate receptor 5 in the amygdala modulates pain-like behavior.
    Authors: Kolber Et al.
    PLoS One  2010;30:8203
  46. 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
  47. Modulator property of the intrinsic cortical projection from layer 6 to layer 4.
    Authors: Lee and Sherman
    Front Syst Neurosci  2009;3:3
  48. Coupling of neural activity to blood flow in olfactory glomeruli is mediated by astrocytic pathways.
    Authors: Petzold Et al.
    Neuropharmacology  2008;58:897
  49. Dichotomous dopaminergic control of striatal synaptic plasticity.
    Authors: Shen Et al.
    Science  2008;321:848
  50. 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
  51. 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
  52. The tyrosine phosphatase STEP mediates AMPA receptor endocytosis after metabotropic glutamate receptor stimulation.
    Authors: Zhang Et al.
    J Neurosci  2008;28:10561
  53. 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
  54. Aberrant early-phase ERK inactivation impedes neuronal function in fragile X syndrome.
    Authors: Kim Et al.
    J Neurosci  2008;105:4429
  55. AMPAR exocytosis through NO modulation of PICK1.
    Authors: Sossa Et al.
    Biol Psychiatry  2007;53:92
  56. Calpain-mediated mGluR1alpha truncation: a key step in excitotoxicity.
    Authors: Xu Et al.
    Neuron  2007;53:399
  57. 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
  58. 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
  59. 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
  60. 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
  61. Ionotropic and metabotropic glutamate receptor antagonism attenuates cue-induced cocaine seeking.
    Authors: Bäckström and Hyytiä
    Neuropsychopharmacology  2006;31:778
  62. 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
  63. Glutamatergic Control of Microvascular Tone by Distinct GABA Neurons in the Cerebellum.
    Authors: Rancillac Et al.
    Neuron  2006;26:6997
  64. Activation of group III metabotropic glutamate receptors attenuates rotenone toxicity on dopaminergic neurons through a microtubule-dependent mechanism.
    Authors: Jiang Et al.
    J Neurosci  2006;26:4318
  65. Stimulation of endocannabinoid formation in brain slice cultures through activation of group I metabotropic glutamate receptors.
    Authors: Jung Et al.
    Neuropsychopharmacology  2005;68:1196
  66. Phospholipase Cbeta serves as a coincidence detector through its Ca2+ dependency for triggering retrograde endocannabinoid signal.
    Authors: Hashimotodani Et al.
    Neuron  2005;45:257
  67. 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
  68. Interactions between ephrin-B and metabotropic glutamate 1 receptors in brain tissue and cultured neurons.
    Authors: Calò Et al.
    J Neurosci  2005;25:2245
  69. Endocannabinoid-mediated metaplasticity in the hippocampus.
    Authors: Chevaleyre and Castillo
    Neuron  2004;43:871
  70. 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
  71. Prefrontal cortex stimulation induces 2-arachidonoyl-glycerol-mediated suppression of excitation in dopamine neurons.
    Authors: Melis Et al.
    J Neurosci  2004;24:10707
  72. 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
  73. Metabotropic mGlu5 receptors regulate adenosine A2A receptor signaling.
    Authors: Nishi Et al.
    J Neurosci  2003;100:1322
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