hmGlu1 subtype-selective non-competitive antagonist (IC50 = 6.5 μM). Has no agonist or antagonist activity at hmGlu2, 4a, 5a, 7b, 8a or ionotropic receptors at concentrations of up to 100 μM.
Sold for research purposes under license from Suntory Ltd.
|Storage||Store at RT|
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|
Preparing Stock Solutions
The following data is based on the product molecular weight 247.25. 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||4.04 mL||20.22 mL||40.44 mL|
|5 mM||0.81 mL||4.04 mL||8.09 mL|
|10 mM||0.4 mL||2.02 mL||4.04 mL|
|50 mM||0.08 mL||0.4 mL||0.81 mL|
References are publications that support the products' biological activity.
Hermans et al (1998) Reversible and non-competitive antagonist profile of CPCCOEt at the human type 1α metabotropic glutamate receptor. Neuropharmacology 37 1645 PMID: 9886688
Litschig et al (1999) CPCCOEt, a noncompetitive metabotropic glutamate receptor 1 antagonist, inhibits receptor signaling without affecting glutamate binding. Mol.Pharmacol. 55 453 PMID: 10051528
If you know of a relevant reference for CPCCOEt, please let us know.
View Related Products by Target
View Related Products by Product Action
Keywords: CPCCOEt, supplier, Selective, non-competitive, mGlu1, mGluR1, receptor, antagonists, Group, I, Receptors, Glutamate, Metabotropic, Glutamate, (Metabotropic), Group, I, Receptors, Glutamate, (Metabotropic), Group, I, Receptors, Tocris Bioscience
17 Citations for CPCCOEt
Citations are publications that use Tocris products. Selected citations for CPCCOEt include:
Cozzoli et al (2012) Nucleus accumbens mGluR5-associated signaling regulates binge alcohol drinking under drinking-in-the-dark procedures. Mol Pain 36 1623 PMID: 22432643
Tappe-Theodor et al (2011) Homer1a signaling in the amygdala counteracts pain-related synaptic plasticity, mGluR1 function and pain behaviors. Proc Natl Acad Sci U S A 7 38 PMID: 21595930
Jackson et al (2010) Control of cerebellar long-term potentiation by P-Rex-family guanine-nucleotide exchange factors and phosphoinositide 3-kinase. PLoS One 5 e11962 PMID: 20694145
Astorga et al (2015) An excitatory GABA loop operating in vivo. Front Cell Neurosci 9 275 PMID: 26236197
Zhong et al (2015) BDNF interacts with endocannabinoids to regulate cocaine-induced synaptic plasticity in mouse midbrain dopamine neurons. Cell Rep 35 4469 PMID: 25762688
Oh et al (2015) Heterosynaptic structural plasticity on local dendritic segments of hippocampal CA1 neurons. Alcohol Clin Exp Res 10 162 PMID: 25558061
Kubota et al (2014) mGluR1-mediated excitation of cerebellar GABAergic interneurons requires both G protein-dependent and Src-ERK1/2-dependent signaling pathways. PLoS One 9 e106316 PMID: 25181481
Tronson et al (2010) Metabotropic glutamate receptor 5/Homer interactions underlie stress effects on fear. J Biol Chem 68 1007 PMID: 21075228
Gibson et al (2008) TRPV1 channels mediate long-term depression at synapses on hippocampal interneurons. Neuron 57 746 PMID: 18341994
Shin et al (2008) Dendritic glutamate release produces autocrine activation of mGluR1 in cerebellar Purkinje cells. J Biol Chem 105 746 PMID: 18174329
Jan and Westbrook (2007) Disynaptic amplification of metabotropic glutamate receptor 1 responses in the olfactory bulb. J Neurosci 27 132 PMID: 17202480
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
El-Kouhen et al (2006) Blockade of mGluR1 receptor results in analgesia and disruption of motor and cognitive performances: effects of A-841720, a novel non-competitive mGluR1 receptor antagonist. Br J Pharmacol 149 761 PMID: 17016515
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. Elife 280 30469 PMID: 15958386
Kawasaki et al (2004) Ionotropic and metabotropic receptors, protein kinase A, protein kinase C, and Src contribute to C-fiber-induced ERK activation and cAMP response element-binding protein phosphorylation in dorsal horn neurons, leading to central sensitization. J Neurosci 24 8310 PMID: 15385614
Kitano et al (2003) Direct interaction and functional coupling between metabotropic glutamate receptor subtype 1 and voltage-sensitive Cav2.1 Ca2+ channel. J Neurosci 278 25101 PMID: 12704197
Do you know of a great paper that uses CPCCOEt from Tocris? If so please let us know.
Average Rating:(Based on 0 Reviews)
Literature in this Area
The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.
Huntington's Disease Poster
Huntington's disease (HD) is a monogenic neurodegenerative disorder, which is characterized by the prevalent loss of GABAergic medium spiny neurons (MSN) in the striatum. This poster summarizes the MSN intracellular signaling pathways implicated in the pathology of HD, as well as highlighting the use of iPSCs for HD modeling.
Learning & Memory Poster
Recognition memory enables us to make judgements about whether or not we have encountered a particular stimulus before. This poster outlines the cellular mechanisms underlying recognition memory and its links to long-term depression, as well as the use of pharmacological intervention to assess the role of neurotransmitters in recognition memory.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.