Catalog Number: 1212
Chemical Name: 2-Methyl-6-(phenylethynyl)pyridine hydrochloride
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:
  • Formula:
  • Solubility:
    Soluble to 5 mM in water with gentle warming and to 100 mM in DMSO
  • Purity:
  • Storage:
    Desiccate at +4°C
  • CAS No:
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.
Background References
  1. Synthesis of S-[3-(4(5)-imidazolyl)propyl]-N-[2-(4-[125I]-iodophenylethyl]isothiourea sulfate [125I]-iodophenpropit), a new probe for histamine H3 receptor binding sites.
    Menge et al.
    J.Labelled Comp.Radiopharm. XXXI, 1992;10:781
  2. 2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist.
    Gasparini et al.
    Neuropharmacology, 1999;38:1493
  3. 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
  4. 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

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

Showing Results 1 - 10 of 51

  1. Augmentation of Ca(2+) signaling in astrocytic endfeet in the latent phase of temporal lobe epilepsy.
    Authors: Szokol Et al.
    Int J Mol Sci
  2. The metabotropic glutamate receptor 5 role on motor behavior involves specific neural substrates.
    Authors: Guimaraes Et al.
    J Biol Chem
  3. 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
  4. Abnormal excitability and episodic low-frequency oscillations in the cerebral cortex of the tottering mouse.
    Authors: Cramer Et al.
    PLoS One
  5. BDNF interacts with endocannabinoids to regulate cocaine-induced synaptic plasticity in mouse midbrain dopamine neurons.
    Authors: Zhong Et al.
    J Neurosci
  6. 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
  7. Nerve demyelination increases metabotropic glutamate receptor subtype 5 expression in peripheral painful mononeuropathy.
    Authors: Ko Et al.
    J Neurophysiol
  8. Both neurons and astrocytes exhibited tetrodotoxin-resistant metabotropic glutamate receptor-dependent spontaneous slow Ca2+ oscillations in striatum.
    Authors: Tamura Et al.
    PLoS One
  9. Effects of the mGluR5 antagonist MPEP on ethanol withdrawal induced anxiety-like syndrome in rats.
    Authors: Kumar Et al.
    Behav Brain Funct
  10. 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
  11. Long lasting protein synthesis- and activity-dependent spine shrinkage and elimination after synaptic depression.
    Authors: Ramiro-Cortés and Israely
    PLoS One
  12. Group II metabotropic glutamate receptors modify N-methyl-D-aspartate receptors via Src kinase.
    Authors: Trepanier Et al.
    Sci Rep
  13. Activation of mGluR5 and inhibition of NADPH oxidase improves functional recovery after traumatic brain injury.
    Authors: Loane Et al.
    J Neurosci
  14. Haploinsufficiency of Cyfip1 produces fragile X-like phenotypes in mice.
    Authors: Bozdagi Et al.
    J Neurosci
  15. Nitrative stress in cerebral endothelium is mediated by mGluR5 in hyperhomocysteinemia.
    Authors: Mayo Et al.
    J Cereb Blood Flow Metab
  16. Central amygdala metabotropic glutamate receptor 5 in the modulation of visceral pain.
    Authors: Crock Et al.
    J Neurotrauma
  17. Developmental regulation of CB1-mediated spike-time dependent depression at immature mossy fiber-CA3 synapses.
    Authors: Caiati Et al.
    Sci Rep
  18. Activity-dependent regulation of synaptic strength by PSD-95 in CA1 neurons.
    Authors: Zhang and Lisman
    J Neurosci
  19. 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
  20. Interactive effects of mGlu5 and 5-HT2A receptors on locomotor activity in mice.
    Authors: Halberstadt Et al.
    Psychopharmacology (Berl)
  21. An excitatory loop with astrocytes contributes to drive neurons to seizure threshold.
    Authors: Gómez-Gonzalo Et al.
    PLoS Biol
  22. Metabotropic glutamate receptor 5/Homer interactions underlie stress effects on fear.
    Authors: Tronson Et al.
    Front Cell Neurosci
  23. The maturation of GABAergic transmission in visual cortex requires endocannabinoid-mediated LTD of inhibitory inputs during a critical period.
    Authors: Jiang Et al.
  24. 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
  25. Distinctions between persistent and reversible group I mGluR-induced epileptiform burst prolongation.
    Authors: Fuortes Et al.
  26. Sensory and cortical activation of distinct glial cell subtypes in the somatosensory thalamus of young rats.
    Authors: Parri Et al.
    Eur J Neurosci
  27. Activation of metabotropic glutamate receptor 5 in the amygdala modulates pain-like behavior.
    Authors: Kolber Et al.
    PLoS One
  28. Discovery of a Novel Chemical Class of mGlu(5) Allosteric Ligands with Distinct Modes of Pharmacology.
    Authors: Hammond Et al.
    ACS Chem Neurosci
  29. Modulator property of the intrinsic cortical projection from layer 6 to layer 4.
    Authors: Lee and Sherman
    Front Syst Neurosci
  30. Coupling of neural activity to blood flow in olfactory glomeruli is mediated by astrocytic pathways.
    Authors: Petzold Et al.
  31. Dichotomous dopaminergic control of striatal synaptic plasticity.
    Authors: Shen Et al.
  32. The tyrosine phosphatase STEP mediates AMPA receptor endocytosis after metabotropic glutamate receptor stimulation.
    Authors: Zhang Et al.
    J Neurosci
  33. 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
  34. Aberrant early-phase ERK inactivation impedes neuronal function in fragile X syndrome.
    Authors: Kim Et al.
    J Neurosci
  35. AMPAR exocytosis through NO modulation of PICK1.
    Authors: Sossa Et al.
    Biol Psychiatry
  36. Calpain-mediated mGluR1alpha truncation: a key step in excitotoxicity.
    Authors: Xu Et al.
  37. Loss of metabotropic glutamate receptor-dependent long-term depression via downregulation of mGluR5 after status epilepticus.
    Authors: Kirschstein Et al.
    J Neurosci
  38. 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
  39. 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
  40. Ionotropic and metabotropic glutamate receptor antagonism attenuates cue-induced cocaine seeking.
    Authors: Bäckström and Hyytiä
  41. Visual experience regulates metabotropic glutamate receptor-mediated plasticity of AMPA receptor synaptic transmission by homer1a induction.
    Authors: Keuren-Jensen and Cline
    J Neurosci
  42. Glutamatergic Control of Microvascular Tone by Distinct GABA Neurons in the Cerebellum.
    Authors: Rancillac Et al.
  43. Stimulation of endocannabinoid formation in brain slice cultures through activation of group I metabotropic glutamate receptors.
    Authors: Jung Et al.
  44. 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
  45. Interactions between ephrin-B and metabotropic glutamate 1 receptors in brain tissue and cultured neurons.
    Authors: Calò Et al.
    J Neurosci
  46. Endocannabinoid-mediated metaplasticity in the hippocampus.
    Authors: Chevaleyre and Castillo
  47. 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
  48. Positive allosteric modulation of the human metabotropic glutamate receptor 4 (hmGluR4) by SIB-1893 and MPEP.
    Authors: Mathiesen Et al.
    Br J Pharmacol
  49. Metabotropic mGlu5 receptors regulate adenosine A2A receptor signaling.
    Authors: Nishi Et al.
    J Neurosci
  50. Cortical layer 1 and layer 2/3 astrocytes exhibit distinct calcium dynamics in vivo.
    Authors: Takata and Hirase
    PLoS One
  51. Molecular components and functions of the endocannabinoid system in mouse prefrontal cortex.
    Authors: Lafourcade Et al.
    PLoS One
Expand to show all
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