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™.
|Storage||Desiccate at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|water||1.15||5mM with gentle warming|
Preparing Stock Solutions
The following data is based on the product molecular weight 229.71. Batch specific molecular weights may vary from batch to batch due to solvent 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|
References are publications that support the products' biological activity.
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
If you know of a relevant reference for MPEP hydrochloride, please let us know.
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Keywords: MPEP hydrochloride, supplier, mGlu5, mGluR5, antagonists, positive, allosteric, modulators, mGlu4, mGluR4, PAM, Positive, Group, I, Receptors, Glutamate, Metabotropic, III, Glutamate, (Metabotropic), Group, I, Receptors, Glutamate, (Metabotropic), Group, III, Receptors, Glutamate, (Metabotropic), Group, I, Receptors, Tocris Bioscience
53 Citations for MPEP hydrochloride
Citations are publications that use Tocris products. Selected citations for MPEP hydrochloride include:
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
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
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 dopamine 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
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
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
Trepanier et al (2013) Group II metabotropic glutamate receptors modify N-methyl-D-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
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
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
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
Zhang and Lisman (2012) Activity-dependent regulation of synaptic strength by PSD-95 in CA1 neurons. J Neurosci 107 1058 PMID: 22114157
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
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
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
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
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
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
Lee and Sherman (2009) Modulator property of the intrinsic cortical projection from layer 6 to layer 4. Front Syst Neurosci 3 3 PMID: 19277215
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
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
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
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
Sossa et al (2007) AMPAR exocytosis through NO modulation of PICK1. Biol Psychiatry 53 92 PMID: 17555774
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
Rancillac et al (2006) Glutamatergic Control of Microvascular Tone by Distinct GABA Neurons in the Cerebellum. Neuron 26 6997 PMID: 16807329
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
Chevaleyre and Castillo (2004) Endocannabinoid-mediated metaplasticity in the hippocampus. Neuron 43 871 PMID: 15363397
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