CPPG

Catalog # Availability Size / Price Qty
0972/5
0972/25
CPPG | CAS No. 183364-82-1 | Group III mGluR Antagonists
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Description: Potent group III mGlu antagonist

Chemical Name: (RS)-α-Cyclopropyl-4-phosphonophenylglycine

Purity: ≥98%

Product Details
Citations (21)
Reviews (2)

Biological Activity

Potent group II/III mGlu receptor antagonist, with approximately 20-fold selectivity for group III over group II (IC50 values of 2.2 and 46.2 nM respectively). A much less potent antagonist at group I receptors in neonatal rat cortical slices (KB = 0.65 ± 0.07 nM). Also available as part of the Group III mGlu Receptor Tocriset™.

Technical Data

M.Wt:
271.21
Formula:
C11H14NO5P
Solubility:
Soluble to 100 mM in 1eq. NaOH
Purity:
≥98%
Storage:
Store at RT
CAS No:
183364-82-1

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.

Background References

  1. Olanzapine: preclinical and clinical profiles of a novel antipsychotic agent.
    Tollefson and Taylor
    CNS Drug Reviews, 2000;6:303
  2. Potent antagonists at L-AP4- and (1S,3S)-ACPD-sensitive presynaptic metabotropic glutamate recpetors in neonatal rat spinal cord.
    Jane et al.
    Neuropharmacology, 1996;35:1029
  3. Potent antagonists at the L-AP4- and (1S, 3S)-ACPD-sensitive presynaptic metabotropic glutamate receptors in the neonatal rat spinal cord.
    Jane et al.
    Neuropharmacology, 1996;35:1029
  4. The effects of (RS)-α-cyclopropyl-4-phosphonophenylglycine ((RS)-CPPG), a potent and selective metabotropic glutamate receptor antagonist.
    Toms et al.
    BrJ.Pharmacol., 1996;119:851
  5. α-Methyl-3-phosphonophenylglycine and α-cyclopropyl-4-phosphonophenylglycine are potent antagonists at mGluRs negatively coupled to adenylyl cyclase.
    Kemp et al.
    Br.J.Pharmacol., 1996;117:(in press)

Product Datasheets

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Citations for CPPG

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

21 Citations: Showing 1 - 10

  1. A group I metabotropic glutamate receptor controls synaptic gain between rods and rod bipolar cells in the mouse retina.
    Authors: Hellmer Et al.
    Physiol Rep  2018;6:e13885
  2. Glutaminolysis drives membrane trafficking to promote invasiveness of breast cancer cells.
    Authors: Dornier
    Nat Commun  2017;8(1):2255
  3. Phasic and Tonic mGlu7 Receptor Activity Modulates the Thalamocortical Network.
    Authors: Tassin Et al.
    Front Neural Circuits  2016;10:31
  4. Glial metabotropic glutamate receptor-4 increases maturation and survival of oligodendrocytes.
    Authors: Spampinato Et al.
    Neurotox Res  2015;8:462
  5. Regulation of output spike patterns by phasic inhibition in cerebellar granule cells.
    Authors: Nieus Et al.
    Front Cell Neurosci  2014;8:246
  6. Examination of VLC-PUFA-deficient photoreceptor terminals.
    Authors: Bennett Et al.
    J Neurosci  2014;55:4063
  7. Group III mGlu receptor agonist, ACPT-I, exerts potential neuroprotective effects in vitro and in vivo.
    Authors: Domin Et al.
    Proc Natl Acad Sci U S A  2014;26:99
  8. Cell type-specific regulation of inhibition via cannabinoid type 1 receptors in rat neocortex.
    Authors: De-May and Ali
    J Neurophysiol  2013;109:216
  9. Increased Kv1 channel expression may contribute to decreased sIPSC frequency following chronic inhibition of NR2B-containing NMDAR.
    Authors: He Et al.
    Neuropsychopharmacology  2012;37:1338
  10. Glutamate controls tPA recycling by astrocytes, which in turn influences glutamatergic signals.
    Authors: Cassé Et al.
    J Neurosci  2012;32:5186
  11. The mode of retinal presynaptic inhibition switches with light intensity.
    Authors: Ichinose and Lukasiewicz
    J Neurosci  2012;32:4360
  12. Antiparkinsonian potential of targeting group III metabotropic glutamate receptor subtypes in the rodent substantia nigra pars reticulata.
    Authors: Broadstock Et al.
    Br J Pharmacol  2012;165:1034
  13. CB1 modulation of temporally distinct synaptic facilitation among local circuit interneurons mediated by N-type calcium channels in CA1.
    Authors: Ali
    J Neurophysiol  2011;105:1051
  14. RGS7 and -11 complexes accelerate the ON-bipolar cell light response.
    Authors: Zhang Et al.
    Invest Ophthalmol Vis Sci  2010;51:1121
  15. Slow glycinergic transmission mediated by transmitter pooling.
    Authors: Balakrishnan Et al.
    Nat Neurosci  2009;12:286
  16. Glutamatergic Control of Microvascular Tone by Distinct GABA Neurons in the Cerebellum.
    Authors: Rancillac Et al.
    J Neurosci  2006;26:6997
  17. 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
  18. Calcium increases in retinal glial cells evoked by light-induced neuronal activity.
    Authors: Newman
    Front Cell Neurosci  2005;25:5502
  19. Positive allosteric modulation of the human metabotropic glutamate receptor 4 (hmGluR4) by SIB-1893 and MPEP.
    Authors: Mathiesen Et al.
    Br J Pharmacol  2003;138:1026
  20. Metabotropic mGlu5 receptors regulate adenosine A2A receptor signaling.
    Authors: Nishi Et al.
    Invest Ophthalmol Vis Sci  2003;100:1322
  21. Neutrophil-derived glutamate regulates vascular endothelial barrier function.
    Authors: Collard Et al.
    J Biol Chem  2002;277:14801

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Used in inhibitor cocktail
By Anonymous on 12/03/2019
Application: Species: Rat

Retinal dissections were performed in HEPES-buffered extracellular solution containing glutamate inhibitor cocktail - 600 umol/L

PMID: 30338673

Use of CPPG as a blocker of mGluRs group III
By Anonymous on 09/17/2019
Application: Species: Rat

CPPG (5 microM) was used for pharmacological isolation of GABA-A receptor activity in nucleated membrane patches. Being added to perfusion solution, CPPG blocked contaminating receptor activity in a recorded response, thus revealing clear GABA-ergic single-channel openings. Figure: single-channel openings of GABA-A receptors in a membrane patch after application of CPPG.

PMID: 30042389

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