Chemical Name: (RS)-α-Cyclopropyl-4-phosphonophenylglycine
Biological ActivityPotent 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™.
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.
Olanzapine: preclinical and clinical profiles of a novel antipsychotic agent.
Tollefson and Taylor
CNS Drug Reviews, 2000;6:303
Potent antagonists at L-AP4- and (1S,3S)-ACPD-sensitive presynaptic metabotropic glutamate recpetors in neonatal rat spinal cord.
Jane et al.
Potent antagonists at the L-AP4- and (1S, 3S)-ACPD-sensitive presynaptic metabotropic glutamate receptors in the neonatal rat spinal cord.
Jane et al.
The effects of (RS)-α-cyclopropyl-4-phosphonophenylglycine ((RS)-CPPG), a potent and selective metabotropic glutamate receptor antagonist.
Toms et al.
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)
Citations for CPPG
The citations listed below are publications that use Tocris products. Selected citations for CPPG include:
21 Citations: Showing 1 - 10
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
Glutaminolysis drives membrane trafficking to promote invasiveness of breast cancer cells.
Nat Commun 2017;8(1):2255
Phasic and Tonic mGlu7 Receptor Activity Modulates the Thalamocortical Network.
Authors: Tassin Et al.
Front Neural Circuits 2016;10:31
Glial metabotropic glutamate receptor-4 increases maturation and survival of oligodendrocytes.
Authors: Spampinato Et al.
Neurotox Res 2015;8:462
Regulation of output spike patterns by phasic inhibition in cerebellar granule cells.
Authors: Nieus Et al.
Front Cell Neurosci 2014;8:246
Examination of VLC-PUFA-deficient photoreceptor terminals.
Authors: Bennett Et al.
J Neurosci 2014;55:4063
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
Cell type-specific regulation of inhibition via cannabinoid type 1 receptors in rat neocortex.
Authors: De-May and Ali
J Neurophysiol 2013;109:216
Increased Kv1 channel expression may contribute to decreased sIPSC frequency following chronic inhibition of NR2B-containing NMDAR.
Authors: He Et al.
Glutamate controls tPA recycling by astrocytes, which in turn influences glutamatergic signals.
Authors: Cassé Et al.
J Neurosci 2012;32:5186
The mode of retinal presynaptic inhibition switches with light intensity.
Authors: Ichinose and Lukasiewicz
J Neurosci 2012;32:4360
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
CB1 modulation of temporally distinct synaptic facilitation among local circuit interneurons mediated by N-type calcium channels in CA1.
J Neurophysiol 2011;105:1051
RGS7 and -11 complexes accelerate the ON-bipolar cell light response.
Authors: Zhang Et al.
Invest Ophthalmol Vis Sci 2010;51:1121
Slow glycinergic transmission mediated by transmitter pooling.
Authors: Balakrishnan Et al.
Nat Neurosci 2009;12:286
Glutamatergic Control of Microvascular Tone by Distinct GABA Neurons in the Cerebellum.
Authors: Rancillac Et al.
J Neurosci 2006;26:6997
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
Calcium increases in retinal glial cells evoked by light-induced neuronal activity.
Front Cell Neurosci 2005;25:5502
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
Metabotropic mGlu5 receptors regulate adenosine A2A receptor signaling.
Authors: Nishi Et al.
Invest Ophthalmol Vis Sci 2003;100:1322
Neutrophil-derived glutamate regulates vascular endothelial barrier function.
Authors: Collard Et al.
J Biol Chem 2002;277:14801
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Retinal dissections were performed in HEPES-buffered extracellular solution containing glutamate inhibitor cocktail - 600 umol/L
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.