Cat. No. 1212
Chemical Name: 2-Methyl-6-(phenylethynyl)pyridine hydrochloride
Biological ActivityPotent 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™.
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.
Certificate of Analysis / Safety Data Sheet
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.
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.
Gasparini et al (1999) 2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist. Neuropharmacology 38 1493. PMID: 10530811.
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.
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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.
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.
Trepanier et al (2013) Group II metabotropic glutamate receptors modify N-methyl-D-aspartate receptors via Src kinase. Sci Rep 3 926. PMID: 23378895.
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.
Mayo et al (2012) Nitrative stress in cerebral endothelium is mediated by mGluR5 in hyperhomocysteinemia. J Cereb Blood Flow Metab 32 825. PMID: 22186670.
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.
Fuortes et al (2010) Distinctions between persistent and reversible group I mGluR-induced epileptiform burst prolongation. Epilepsia 51 1633. PMID: 20659148.
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.
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.
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.
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.
Lee and Sherman (2009) Modulator property of the intrinsic cortical projection from layer 6 to layer 4. Front Syst Neurosci 3 3. PMID: 19277215.
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.
Shen et al (2008) Dichotomous dopaminergic 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.
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.
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.
Xu et al (2007) Calpain-mediated mGluR1alpha truncation: a key step in excitotoxicity. Neuron 53 399. PMID: 17270736.
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.
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.
Chevaleyre and Castillo (2004) Endocannabinoid-mediated metaplasticity in the hippocampus. Neuron 43 871. PMID: 15363397.
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.
Lafourcade et al Molecular components and functions of the endocannabinoid system in mouse prefrontal cortex. PLoS One 2 e709. PMID: 17684555.
Takata and Hirase Cortical layer 1 and layer 2/3 astrocytes exhibit distinct calcium dynamics in vivo. PLoS One 3 e2525. PMID: 18575586.
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Keywords: MPEP hydrochloride, supplier, mGlu5, mGluR5, antagonists, positive, allosteric, modulators, mGlu4, mGluR4, PAM, Positive, Group, I, Receptors, Glutamate, Metabotropic, III, Tocris Bioscience, Glutamate (Metabotropic) Group I Receptor Antagonist products
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