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company name :
Tocris Bioscience
product type :
chemical
product name :
1212/10
catalog :
1212/10
quantity :
10 mg (also 50 mg)
price :
198 USD
more info or order :
citations: 91
Reference
Birdsong W, Jongbloets B, Engeln K, Wang D, Scherrer G, Mao T. Synapse-specific opioid modulation of thalamo-cortico-striatal circuits. elife. 2019;8: pubmed publisher
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Hashimotodani Y, Nasrallah K, Jensen K, Chavez A, Carrera D, Castillo P. LTP at Hilar Mossy Cell-Dentate Granule Cell Synapses Modulates Dentate Gyrus Output by Increasing Excitation/Inhibition Balance. Neuron. 2017;95:928-943.e3 pubmed publisher
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David Pereira A, Sagalajev B, Wei H, Almeida A, Pertovaara A, Pinto Ribeiro F. The medullary dorsal reticular nucleus as a relay for descending pronociception induced by the mGluR5 in the rat infralimbic cortex. Neuroscience. 2017;349:341-354 pubmed publisher
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Rizwan A, Zhan X, Zamponi G, Turner R. Long-Term Potentiation at the Mossy Fiber-Granule Cell Relay Invokes Postsynaptic Second-Messenger Regulation of Kv4 Channels. J Neurosci. 2016;36:11196-11207 pubmed
Choi C, Schoenfeld B, Bell A, Hinchey J, Rosenfelt C, Gertner M, et al. Multiple Drug Treatments That Increase cAMP Signaling Restore Long-Term Memory and Aberrant Signaling in Fragile X Syndrome Models. Front Behav Neurosci. 2016;10:136 pubmed publisher
Guo W, Molinaro G, Collins K, Hays S, Paylor R, Worley P, et al. Selective Disruption of Metabotropic Glutamate Receptor 5-Homer Interactions Mimics Phenotypes of Fragile X Syndrome in Mice. J Neurosci. 2016;36:2131-47 pubmed publisher
Sethna F, Wang H. Acute inhibition of mGluR5 disrupts behavioral flexibility. Neurobiol Learn Mem. 2016;130:1-6 pubmed publisher
Pallo S, DiMaio J, Cook A, Nilsson B, Johnson G. Mechanisms of tau and Aβ-induced excitotoxicity. Brain Res. 2016;1634:119-131 pubmed publisher
Hullinger R, O Riordan K, Burger C. 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. Neurobiol Learn Mem. 2015;125:126-34 pubmed publisher
Kalinowska M, Chávez A, Lutzu S, Castillo P, Bukauskas F, Francesconi A. Actinin-4 Governs Dendritic Spine Dynamics and Promotes Their Remodeling by Metabotropic Glutamate Receptors. J Biol Chem. 2015;290:15909-20 pubmed publisher
Guimaraes I, Carvalho T, Ferguson S, Pereira G, Ribeiro F. The metabotropic glutamate receptor 5 role on motor behavior involves specific neural substrates. Mol Brain. 2015;8:24 pubmed publisher
Cramer S, Popa L, Carter R, Chen G, Ebner T. Abnormal excitability and episodic low-frequency oscillations in the cerebral cortex of the tottering mouse. J Neurosci. 2015;35:5664-79 pubmed publisher
Szokol K, Heuser K, Tang W, Jensen V, Enger R, Bedner P, et al. Augmentation of Ca(2+) signaling in astrocytic endfeet in the latent phase of temporal lobe epilepsy. Front Cell Neurosci. 2015;9:49 pubmed publisher
Zhong P, Liu Y, Hu Y, Wang T, Zhao Y, Liu Q. BDNF interacts with endocannabinoids to regulate cocaine-induced synaptic plasticity in mouse midbrain dopamine neurons. J Neurosci. 2015;35:4469-81 pubmed publisher
Tang A, Alger B. Homer protein-metabotropic glutamate receptor binding regulates endocannabinoid signaling and affects hyperexcitability in a mouse model of fragile X syndrome. J Neurosci. 2015;35:3938-45 pubmed publisher
Ko M, Hsieh Y, Hsieh S, Tseng T. Nerve demyelination increases metabotropic glutamate receptor subtype 5 expression in peripheral painful mononeuropathy. Int J Mol Sci. 2015;16:4642-65 pubmed publisher
Galván E, Pérez Rosello T, Gómez Lira G, Lara E, Gutiérrez R, Barrionuevo G. Synapse-specific compartmentalization of signaling cascades for LTP induction in CA3 interneurons. Neuroscience. 2015;290:332-45 pubmed publisher
Xu J, Antion M, Nomura T, Kraniotis S, Zhu Y, Contractor A. Hippocampal metaplasticity is required for the formation of temporal associative memories. J Neurosci. 2014;34:16762-73 pubmed publisher
Rook J, Tantawy M, Ansari M, Felts A, Stauffer S, Emmitte K, et al. Relationship between in vivo receptor occupancy and efficacy of metabotropic glutamate receptor subtype 5 allosteric modulators with different in vitro binding profiles. Neuropsychopharmacology. 2015;40:755-65 pubmed publisher
Tamura A, Yamada N, Yaguchi Y, Machida Y, Mori I, Osanai M. Both neurons and astrocytes exhibited tetrodotoxin-resistant metabotropic glutamate receptor-dependent spontaneous slow Ca2+ oscillations in striatum. PLoS ONE. 2014;9:e85351 pubmed publisher
Kumar J, Hapidin H, Bee Y, Ismail Z. Effects of the mGluR5 antagonist MPEP on ethanol withdrawal induced anxiety-like syndrome in rats. Behav Brain Funct. 2013;9:43 pubmed publisher
Kuribayashi N, Uchida D, Kinouchi M, Takamaru N, Tamatani T, Nagai H, et al. The role of metabotropic glutamate receptor 5 on the stromal cell-derived factor-1/CXCR4 system in oral cancer. PLoS ONE. 2013;8:e80773 pubmed publisher
Keck T, Zou M, Bi G, Zhang H, Wang X, Yang H, et al. A novel mGluR5 antagonist, MFZ 10-7, inhibits cocaine-taking and cocaine-seeking behavior in rats. Addict Biol. 2014;19:195-209 pubmed publisher
Ramiro Cortés Y, Israely I. Long lasting protein synthesis- and activity-dependent spine shrinkage and elimination after synaptic depression. PLoS ONE. 2013;8:e71155 pubmed publisher
Clem R, Huganir R. Norepinephrine enhances a discrete form of long-term depression during fear memory storage. J Neurosci. 2013;33:11825-32 pubmed publisher
Martinez Rivera A, Rodríguez Borrero E, Matías Alemán M, Montalvo Acevedo A, Guerrero Figuereo K, Febo Rodríguez L, et al. Metabotropic glutamate receptor 5 within nucleus accumbens shell modulates environment-elicited cocaine conditioning expression. Pharmacol Biochem Behav. 2013;110:154-60 pubmed publisher
Zhang Z, Cordeiro Matos S, Jego S, Adamantidis A, Séguéla P. Norepinephrine drives persistent activity in prefrontal cortex via synergistic ?1 and ?2 adrenoceptors. PLoS ONE. 2013;8:e66122 pubmed publisher
Trepanier C, Lei G, Xie Y, MacDonald J. Group II metabotropic glutamate receptors modify N-methyl-D-aspartate receptors via Src kinase. Sci Rep. 2013;3:926 pubmed publisher
Oh W, Hill T, Zito K. Synapse-specific and size-dependent mechanisms of spine structural plasticity accompanying synaptic weakening. Proc Natl Acad Sci U S A. 2013;110:E305-12 pubmed publisher
Loane D, Stoica B, Byrnes K, Jeong W, Faden A. Activation of mGluR5 and inhibition of NADPH oxidase improves functional recovery after traumatic brain injury. J Neurotrauma. 2013;30:403-12 pubmed publisher
Péterfi Z, Urbán G, Papp O, Németh B, Monyer H, Szabó G, et al. Endocannabinoid-mediated long-term depression of afferent excitatory synapses in hippocampal pyramidal cells and GABAergic interneurons. J Neurosci. 2012;32:14448-63 pubmed publisher
Crock L, Kolber B, Morgan C, Sadler K, Vogt S, Bruchas M, et al. Central amygdala metabotropic glutamate receptor 5 in the modulation of visceral pain. J Neurosci. 2012;32:14217-26 pubmed publisher
Bozdagi O, Sakurai T, Dorr N, Pilorge M, Takahashi N, Buxbaum J. Haploinsufficiency of Cyfip1 produces fragile X-like phenotypes in mice. PLoS ONE. 2012;7:e42422 pubmed publisher
He L, Linden D, Sapirstein A. Astrocyte inositol triphosphate receptor type 2 and cytosolic phospholipase A2 alpha regulate arteriole responses in mouse neocortical brain slices. PLoS ONE. 2012;7:e42194 pubmed publisher
Fox J, Sakamuru S, Huang R, Teneva N, Simmons S, Xia M, et al. High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death. Proc Natl Acad Sci U S A. 2012;109:5423-8 pubmed publisher
Caiati M, Sivakumaran S, Lanore F, Mulle C, Richard E, Verrier D, et al. Developmental regulation of CB1-mediated spike-time dependent depression at immature mossy fiber-CA3 synapses. Sci Rep. 2012;2:285 pubmed publisher
Beard R, Reynolds J, Bearden S. Metabotropic glutamate receptor 5 mediates phosphorylation of vascular endothelial cadherin and nuclear localization of ?-catenin in response to homocysteine. Vascul Pharmacol. 2012;56:159-67 pubmed publisher
Mayo J, Beard R, Price T, Chen C, Erickson M, Ercal N, et al. Nitrative stress in cerebral endothelium is mediated by mGluR5 in hyperhomocysteinemia. J Cereb Blood Flow Metab. 2012;32:825-34 pubmed publisher
Giordano C, Cristino L, Luongo L, Siniscalco D, Petrosino S, Piscitelli F, et al. TRPV1-dependent and -independent alterations in the limbic cortex of neuropathic mice: impact on glial caspases and pain perception. Cereb Cortex. 2012;22:2495-518 pubmed publisher
Zhang P, Lisman J. Activity-dependent regulation of synaptic strength by PSD-95 in CA1 neurons. J Neurophysiol. 2012;107:1058-66 pubmed publisher
Hays S, Huber K, Gibson J. Altered neocortical rhythmic activity states in Fmr1 KO mice are due to enhanced mGluR5 signaling and involve changes in excitatory circuitry. J Neurosci. 2011;31:14223-34 pubmed publisher
Zheng N, Raman I. Prolonged postinhibitory rebound firing in the cerebellar nuclei mediated by group I metabotropic glutamate receptor potentiation of L-type calcium currents. J Neurosci. 2011;31:10283-92 pubmed publisher
Chen M, Wan Y, ADE K, Ting J, Feng G, Calakos N. Sapap3 deletion anomalously activates short-term endocannabinoid-mediated synaptic plasticity. J Neurosci. 2011;31:9563-73 pubmed publisher
Halberstadt A, Lehmann Masten V, Geyer M, Powell S. Interactive effects of mGlu5 and 5-HT2A receptors on locomotor activity in mice. Psychopharmacology (Berl). 2011;215:81-92 pubmed publisher
Price D, Rockenstein E, Ubhi K, Phung V, MacLean Lewis N, Askay D, et al. Alterations in mGluR5 expression and signaling in Lewy body disease and in transgenic models of alpha-synucleinopathy--implications for excitotoxicity. PLoS ONE. 2010;5:e14020 pubmed publisher
Tronson N, Guzman Y, Guedea A, Huh K, Gao C, Schwarz M, et al. Metabotropic glutamate receptor 5/Homer interactions underlie stress effects on fear. Biol Psychiatry. 2010;68:1007-15 pubmed publisher
Hammond A, Rodriguez A, Townsend S, Niswender C, Gregory K, Lindsley C, et al. Discovery of a Novel Chemical Class of mGlu(5) Allosteric Ligands with Distinct Modes of Pharmacology. ACS Chem Neurosci. 2010;1:702-716 pubmed
Fuortes M, Rico M, Merlin L. Distinctions between persistent and reversible group I mGluR-induced epileptiform burst prolongation. Epilepsia. 2010;51:1633-7 pubmed publisher
Parri H, Gould T, Crunelli V. Sensory and cortical activation of distinct glial cell subtypes in the somatosensory thalamus of young rats. Eur J Neurosci. 2010;32:29-40 pubmed publisher
Foong J, Bornstein J. mGluR(1) Receptors Contribute to Non-Purinergic Slow Excitatory Transmission to Submucosal VIP Neurons of Guinea-Pig Ileum. Front Neurosci. 2009;3:46 pubmed publisher
Kolber B, Montana M, Carrasquillo Y, Xu J, Heinemann S, Muglia L, et al. Activation of metabotropic glutamate receptor 5 in the amygdala modulates pain-like behavior. J Neurosci. 2010;30:8203-13 pubmed publisher
Jiang B, Huang S, De Pasquale R, Millman D, Song L, Lee H, et al. The maturation of GABAergic transmission in visual cortex requires endocannabinoid-mediated LTD of inhibitory inputs during a critical period. Neuron. 2010;66:248-59 pubmed publisher
Gomez Gonzalo M, Losi G, Chiavegato A, Zonta M, Cammarota M, Brondi M, et al. An excitatory loop with astrocytes contributes to drive neurons to seizure threshold. PLoS Biol. 2010;8:e1000352 pubmed publisher
Kato H, Watabe A, Manabe T. Non-Hebbian synaptic plasticity induced by repetitive postsynaptic action potentials. J Neurosci. 2009;29:11153-60 pubmed publisher
Lee C, Sherman S. Modulator property of the intrinsic cortical projection from layer 6 to layer 4. Front Syst Neurosci. 2009;3:3 pubmed publisher
Ferguson A, Bolding K, Huie J, Hook M, Santillano D, Miranda R, et al. Group I metabotropic glutamate receptors control metaplasticity of spinal cord learning through a protein kinase C-dependent mechanism. J Neurosci. 2008;28:11939-49 pubmed publisher
Zhang Y, Venkitaramani D, Gladding C, Zhang Y, Kurup P, Molnar E, et al. The tyrosine phosphatase STEP mediates AMPA receptor endocytosis after metabotropic glutamate receptor stimulation. J Neurosci. 2008;28:10561-6 pubmed publisher
Grueter B, McElligott Z, ROBISON A, Mathews G, Winder D. In vivo metabotropic glutamate receptor 5 (mGluR5) antagonism prevents cocaine-induced disruption of postsynaptically maintained mGluR5-dependent long-term depression. J Neurosci. 2008;28:9261-70 pubmed publisher
Shen W, Flajolet M, Greengard P, Surmeier D. Dichotomous dopaminergic control of striatal synaptic plasticity. Science. 2008;321:848-51 pubmed publisher
Huang Y, Yasuda H, Sarihi A, Tsumoto T. Roles of endocannabinoids in heterosynaptic long-term depression of excitatory synaptic transmission in visual cortex of young mice. J Neurosci. 2008;28:7074-83 pubmed publisher
Petzold G, Albeanu D, Sato T, Murthy V. Coupling of neural activity to blood flow in olfactory glomeruli is mediated by astrocytic pathways. Neuron. 2008;58:897-910 pubmed publisher
Takata N, Hirase H. Cortical layer 1 and layer 2/3 astrocytes exhibit distinct calcium dynamics in vivo. PLoS ONE. 2008;3:e2525 pubmed publisher
Neyman S, Manahan Vaughan D. 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. 2008;27:1345-52 pubmed publisher
Kim S, Markham J, Weiler I, Greenough W. Aberrant early-phase ERK inactivation impedes neuronal function in fragile X syndrome. Proc Natl Acad Sci U S A. 2008;105:4429-34 pubmed publisher
Nakamoto M, Nalavadi V, Epstein M, Narayanan U, Bassell G, Warren S. Fragile X mental retardation protein deficiency leads to excessive mGluR5-dependent internalization of AMPA receptors. Proc Natl Acad Sci U S A. 2007;104:15537-42 pubmed
Lafourcade M, Elezgarai I, Mato S, Bakiri Y, Grandes P, Manzoni O. Molecular components and functions of the endocannabinoid system in mouse prefrontal cortex. PLoS ONE. 2007;2:e709 pubmed
Kirschstein T, Bauer M, Müller L, Rüschenschmidt C, Reitze M, Becker A, et al. Loss of metabotropic glutamate receptor-dependent long-term depression via downregulation of mGluR5 after status epilepticus. J Neurosci. 2007;27:7696-704 pubmed
Sossa K, Beattie J, Carroll R. AMPAR exocytosis through NO modulation of PICK1. Neuropharmacology. 2007;53:92-100 pubmed
Muddashetty R, Kelic S, Gross C, Xu M, Bassell G. 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. 2007;27:5338-48 pubmed
Xu W, Wong T, Chery N, Gaertner T, Wang Y, Baudry M. Calpain-mediated mGluR1alpha truncation: a key step in excitotoxicity. Neuron. 2007;53:399-412 pubmed
Bloodgood B, Sabatini B. Nonlinear regulation of unitary synaptic signals by CaV(2.3) voltage-sensitive calcium channels located in dendritic spines. Neuron. 2007;53:249-60 pubmed
Van Keuren Jensen K, Cline H. Visual experience regulates metabotropic glutamate receptor-mediated plasticity of AMPA receptor synaptic transmission by homer1a induction. J Neurosci. 2006;26:7575-80 pubmed
Rancillac A, Rossier J, Guille M, Tong X, Geoffroy H, Amatore C, et al. Glutamatergic Control of Microvascular Tone by Distinct GABA Neurons in the Cerebellum. J Neurosci. 2006;26:6997-7006 pubmed
Jiang Q, Yan Z, Feng J. Activation of group III metabotropic glutamate receptors attenuates rotenone toxicity on dopaminergic neurons through a microtubule-dependent mechanism. J Neurosci. 2006;26:4318-28 pubmed
Bäckström P, Hyytia P. Ionotropic and metabotropic glutamate receptor antagonism attenuates cue-induced cocaine seeking. Neuropsychopharmacology. 2006;31:778-86 pubmed
Jung K, Mangieri R, Stapleton C, Kim J, Fegley D, Wallace M, et al. Stimulation of endocannabinoid formation in brain slice cultures through activation of group I metabotropic glutamate receptors. Mol Pharmacol. 2005;68:1196-202 pubmed
Jong Y, Kumar V, Kingston A, Romano C, O Malley K. Functional metabotropic glutamate receptors on nuclei from brain and primary cultured striatal neurons. Role of transporters in delivering ligand. J Biol Chem. 2005;280:30469-80 pubmed
Calo L, Bruno V, Spinsanti P, Molinari G, Korkhov V, Esposito Z, et al. Interactions between ephrin-B and metabotropic glutamate 1 receptors in brain tissue and cultured neurons. J Neurosci. 2005;25:2245-54 pubmed
Hashimotodani Y, Ohno Shosaku T, Tsubokawa H, Ogata H, Emoto K, Maejima T, et al. Phospholipase Cbeta serves as a coincidence detector through its Ca2+ dependency for triggering retrograde endocannabinoid signal. Neuron. 2005;45:257-68 pubmed
Melis M, Perra S, Muntoni A, Pillolla G, Lutz B, Marsicano G, et al. Prefrontal cortex stimulation induces 2-arachidonoyl-glycerol-mediated suppression of excitation in dopamine neurons. J Neurosci. 2004;24:10707-15 pubmed
Chevaleyre V, Castillo P. Endocannabinoid-mediated metaplasticity in the hippocampus. Neuron. 2004;43:871-81 pubmed
Gallagher S, Daly C, Bear M, Huber K. Extracellular signal-regulated protein kinase activation is required for metabotropic glutamate receptor-dependent long-term depression in hippocampal area CA1. J Neurosci. 2004;24:4859-64 pubmed
Wu M, Hajszan T, Xu C, Leranth C, Alreja M. Group I metabotropic glutamate receptor activation produces a direct excitation of identified septohippocampal cholinergic neurons. J Neurophysiol. 2004;92:1216-25 pubmed
Mathiesen J, Svendsen N, Brauner Osborne H, Thomsen C, Ramirez M. Positive allosteric modulation of the human metabotropic glutamate receptor 4 (hmGluR4) by SIB-1893 and MPEP. Br J Pharmacol. 2003;138:1026-30 pubmed
Nishi A, Liu F, Matsuyama S, Hamada M, Higashi H, Nairn A, et al. Metabotropic mGlu5 receptors regulate adenosine A2A receptor signaling. Proc Natl Acad Sci U S A. 2003;100:1322-7 pubmed
product information
master code :
1212
SKU :
1212/10
product name :
MPEP hydrochloride
unit size :
10 mg (also 50 mg)
description :
Potent mGlu5 antagonist; also positive allosteric modulator of mGlu4 receptors
target :
Group I mGluR Antagonists
category :
Small Molecules
purity :
99%
observed molecular weight :
229.71
url print :
?utm_source=labome&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules
details of functionality :
MPEP hydrochloride is a 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.
top caption :
Potent mGlu5 antagonist; also positive allosteric modulator of mGlu4 receptors
extended description :
Potent mGlu5 antagonist; also positive allosteric modulator of mGlu4 receptors
chemical name text :
2-Methyl-6-(phenylethynyl)pyridine hydrochloride
formula :
C14H11N.HCl
formula text :
C14H11N.HCl
cas num :
219911-35-0
USD :
198 USD
product details :
Potent mGlu5 antagonist; also positive allosteric modulator of mGlu4 receptors
storage :
Desiccate at +4░C
more info or order :
company information
Tocris Bioscience
The Watkins Building
Atlantic Road
Avonmouth, Bristol
BS11 9QD
info@bio-techne.com
https://www.tocris.com
800-343-7475
headquarters: UK