Home / Group I mGluR Antagonists / CPCCOEt

CPCCOEt

Catalog #: 1028
28 Citations 1 Review Datasheet / COA / SDS
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1028/50
CPCCOEt | CAS No. 179067-99-3 | Group I mGluR Antagonists
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Description: Selective non-competitive mGlu1 antagonist

Chemical Name: 7-(Hydroxyimino)cyclopropa[b]chromen-1a-carboxylate ethyl ester

Purity: ≥99%

Product Details
Citations (28)
Supplemental Products
Reviews (1)
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

CPCCOEt is a 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.

Technical Data

M.Wt:
247.25
Formula:
C13H13NO4
Solubility:
Soluble to 5 mM in ethanol and to 100 mM in DMSO
Purity:
≥99%
Storage:
Store at RT
CAS No:
179067-99-3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold for research purposes under license from Suntory Ltd.

Background References

  1. Osteosarcoma cell proliferation and survival requires mGluR5 receptor activity and is blocked by Riluzole
    S Liao, Y Ruiz, H Gulzar, Z Yelskaya, L Ait Taouit, M Houssou, T Jaikaran, Y Schvarts, K Kozlitina, U Basu-Roy, A Mansukhani, SS Mahajan
    PLoS ONE, 2017;12(2):e0171256.
  2. High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
    Fox JT, Sakamuru S, Huang R
    Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8.
  3. Reversible and non-competitive antagonist profile of CPCCOEt at the human type 1α metabotropic glutamate receptor.
    Hermans et al.
    Neuropharmacology, 1998;37:1645
  4. CPCCOEt, a noncompetitive metabotropic glutamate receptor 1 antagonist, inhibits receptor signaling without affecting glutamate binding.
    Litschig et al.
    Mol.Pharmacol., 1999;55:453
  5. A novel class of antagonists for metabotropic glutamate receptors, 7-(hydroxyimino)cyclopropa[b]chromen-1a-carboxylates.
    Annoura et al.
    Bioorg.Med.Chem.Lett., 1996;6:763

Product Datasheets

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Citations for CPCCOEt

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

28 Citations: Showing 1 - 10

  1. DA Cells Differentially Regulate Striatal Cholinergic Transmission across Regions through Corelease of DA and Glutamate.
    Authors: Cai and Ford
    Cell Rep  2018;25:3148
  2. An excitatory GABA loop operating in vivo.
    Authors: Astorga Et al.
    Front Cell Neurosci  2015;9:275
  3. BDNF interacts with endocannabinoids to regulate cocaine-induced synaptic plasticity in mouse midbrain DA neurons.
    Authors: Zhong Et al.
    Cell Rep  2015;35:4469
  4. Heterosynaptic structural plasticity on local dendritic segments of hippocampal CA1 neurons.
    Authors: Oh Et al.
    Alcohol Clin Exp Res  2015;10:162
  5. mGluR1-mediated excitation of cerebellar GABAergic interneurons requires both G protein-dependent and Src-ERK1/2-dependent signaling pathways.
    Authors: Kubota Et al.
    PLoS One  2014;9:e106316
  6. Synapse-specific and size-dependent mechanisms of spine structural plasticity accompanying synaptic weakening.
    Authors: Oh Et al.
    Proc Natl Acad Sci U S A  2013;110:E305
  7. Nucleus accumbens mGluR5-associated signaling regulates binge alcohol drinking under drinking-in-the-dark procedures.
    Authors: Cozzoli Et al.
    Mol Pain  2012;36:1623
  8. Homer1a signaling in the amygdala counteracts pain-related synaptic plasticity, mGluR1 function and pain behaviors.
    Authors: Tappe-Theodor Et al.
    Proc Natl Acad Sci U S A  2011;7:38
  9. Prolonged postinhibitory rebound firing in the cerebellar nuclei mediated by group I metabotropic glutamate receptor potentiation of L-type calcium currents.
    Authors: Zheng and Raman
    J Neurosci  2011;31:10283
  10. Metabotropic glutamate receptor 5/Homer interactions underlie stress effects on fear.
    Authors: Tronson Et al.
    J Biol Chem  2010;68:1007
  11. Control of cerebellar long-term potentiation by P-Rex-family guanine-nucleotide exchange factors and phosphoinositide 3-kinase.
    Authors: Jackson Et al.
    PLoS One  2010;5:e11962
  12. Mobilization of calcium from intracellular stores facilitates somatodendritic DA release.
    Authors: Patel Et al.
    J Neurosci  2009;29:6568
  13. TRPV1 channels mediate long-term depression at synapses on hippocampal interneurons.
    Authors: Gibson Et al.
    Neuron  2008;57:746
  14. Dendritic glutamate release produces autocrine activation of mGluR1 in cerebellar Purkinje cells.
    Authors: Shin Et al.
    J Biol Chem  2008;105:746
  15. Nonlinear regulation of unitary synaptic signals by CaV(2.3) voltage-sensitive calcium channels located in dendritic spines.
    Authors: Bloodgood and Sabatini
    Neuron  2007;53:249
  16. Loss of metabotropic glutamate receptor-dependent long-term depression via downregulation of mGluR5 after status epilepticus.
    Authors: Kirschstein Et al.
    J Neurosci  2007;27:7696
  17. Disynaptic amplification of metabotropic glutamate receptor 1 responses in the olfactory bulb.
    Authors: Jan and Westbrook
    J Neurosci  2007;27:132
  18. Somatodendritic release of glutamate regulates synaptic inhibition in cerebellar Purkinje cells via autocrine mGluR1 activation.
    Authors: Duguid Et al.
    J Neurosci  2007;27:12464
  19. Activation of group III metabotropic glutamate receptors attenuates rotenone toxicity on DArgic neurons through a microtubule-dependent mechanism.
    Authors: Jiang Et al.
    J Neurosci  2006;26:4318
  20. 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.
    Authors: El-Kouhen Et al.
    Br J Pharmacol  2006;149:761
  21. Phospholipase Cbeta serves as a coincidence detector through its Ca2+ dependency for triggering retrograde endocannabinoid signal.
    Authors: Hashimotodani Et al.
    Neuron  2005;45:257
  22. Functional metabotropic glutamate receptors on nuclei from brain and primary cultured striatal neurons. Role of transporters in delivering ligand.
    Authors: Jong Et al.
    Elife  2005;280:30469
  23. Interactions between ephrin-B and metabotropic glutamate 1 receptors in brain tissue and cultured neurons.
    Authors: Calò Et al.
    J Neurosci  2005;25:2245
  24. Group I metabotropic glutamate receptor activation produces a direct excitation of identified septohippocampal cholinergic neurons.
    Authors: Wu Et al.
    J Neurophysiol  2004;92:1216
  25. 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.
    Authors: Kawasaki Et al.
    J Neurosci  2004;24:8310
  26. Prefrontal cortex stimulation induces 2-arachidonoyl-glycerol-mediated suppression of excitation in DA neurons.
    Authors: Melis Et al.
    J Neurosci  2004;24:10707
  27. Direct interaction and functional coupling between metabotropic glutamate receptor subtype 1 and voltage-sensitive Cav2.1 Ca2+ channel.
    Authors: Kitano Et al.
    J Neurosci  2003;278:25101
  28. Allosteric modulation of group III metabotropic glutamate receptor 4: a potential approach to Parkinson's disease treatment.
    Authors: Marino Et al.
    Proc Natl Acad Sci U S A  2003;100:13668

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Succesfull block of mGluRs
By Anonymous on 11/02/2017

We use bath application of CPCCOEt and MPEP to block mGluRs.

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