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Submit ReviewCGP 52432
Description: Potent and selective GABAB antagonist
Chemical Name: 3-[[(3,4-Dichlorophenyl)methyl]amino]propyl] diethoxymethyl)phosphinic acid
Purity: ≥98% (HPLC)
Biological Activity for CGP 52432
CGP 52432 is a potent, selective GABAB receptor antagonist (IC50 = 85 nM).
Licensing Information
Sold with the permission of Novartis Pharma AG
Technical Data for CGP 52432
| M. Wt | 384.24 |
| Formula | C15H24Cl2NO4P |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 139667-74-6 |
| PubChem ID | 132252 |
| InChI Key | GJZVQXWEIYRHBE-UHFFFAOYSA-N |
| Smiles | ClC1=CC=C(CNCCCP(C(OCC)OCC)(O)=O)C=C1Cl |
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.
Solubility Data for CGP 52432
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 1.92 | 5 |
Preparing Stock Solutions for CGP 52432
The following data is based on the product molecular weight 384.24. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.05 mM | 52.05 mL | 260.25 mL | 520.51 mL |
| 0.25 mM | 10.41 mL | 52.05 mL | 104.1 mL |
| 0.5 mM | 5.21 mL | 26.03 mL | 52.05 mL |
| 2.5 mM | 1.04 mL | 5.21 mL | 10.41 mL |
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Product Datasheets for CGP 52432
References for CGP 52432
References are publications that support the biological activity of the product.
Bonanno et al (1998) GABAB receptors as potential targets for drugs able to prevent excessive excitatory amino acid transmission in the spinal cord. Eur.J.Pharmacol. 362 143 PMID: 9874164
Lanza et al (1993) CGP 52432: a novel potent and selective GABAB autoreceptor antagonist in rat cerebral cortex. Eur.J.Pharmacol. 237 191 PMID: 8103461
Libri et al (1998) Blockade of GABAB receptors facilitates muscarinic agonist-induced epileptiform activity in immature rat piriform cortex in vitro. Naunyn Schmiedebergs Arch.Pharmacol. 358 168 PMID: 9750001
Froestl et al (1996) Potent, orally active GABAB receptor antagonists. Pharmacol.Rev.Comm. 8 127
If you know of a relevant reference for CGP 52432, please let us know.
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Keywords: CGP 52432, CGP 52432 supplier, Potent, selective, GABAB, antagonists, Receptors, CGP52432, 1246, Tocris Bioscience
22 Citations for CGP 52432
Citations are publications that use Tocris products. Selected citations for CGP 52432 include:
Parker et al (2011) Attenuating GABA(A) receptor signaling in DA neurons selectively enhances reward learning and alters risk preference in mice. J Neurosci 31 17103 PMID: 22114279
Moore et al (2009) Plasticity of burst firing induced by synergistic activation of metabotropic glutamate and acetylcholine receptors. Neuron 61 287 PMID: 19186170
Song et al (2013) Different transporter systems regulate extracellular GABA from vesicular and non-vesicular sources. Front Cell Neurosci 7 23 PMID: 23494150
Venkataraman and Bartlett (2013) Postnatal development of synaptic properties of the GABAergic projection from the inferior colliculus to the auditory thalamus. J Neurophysiol 109 2866 PMID: 23536710
Li et al (2011) Synergistic activation of DA D1 and TrkB receptors mediate gain control of synaptic plasticity in the basolateral amygdala. PLoS One 6 e26065 PMID: 22022509
Xiao et al (2012) The role of inhibition in oscillatory wave dynamics in the cortex. Eur J Neurosci 36 2201 PMID: 22805065
Adedoyin et al (2010) Endogenous N-acetylaspartylglutamate (NAAG) inhibits synaptic plasticity/transmission in the amygdala in a mouse inflammatory pain model. Mol Pain 6 60 PMID: 20860833
Jung Kim et al (2016) Vasculo-neuronal coupling: retrograde vascular communication to brain neurons The Journal of Neuroscience 14 12624 PMID: 27821575
Sargin et al (2016) Chronic social isolation reduces 5-HT neuronal activity via upregulated SK3 calcium-activated potassium channels Elife 5 e21416 PMID: 27874831
Yang et al (2013) PropF. inhibits superoxide production, elastase release, and chemotaxis in formyl peptide-activated human neutrophils by blocking formyl peptide receptor 1. J Immunol 190 6511 PMID: 23670191
Caiati et al (2012) Developmental regulation of CB1-mediated spike-time dependent depression at immature mossy fiber-CA3 synapses. Sci Rep 2 285 PMID: 22368777
Dobson et al (2015) Caffeine Modulates Vesicle Release and Recovery at Cerebellar Parallel Fibre Terminals, Independently of Calcium and Cyclic AMP Signalling. J Pharmacol Exp Ther 10 e0125974 PMID: 25933382
Wu et al (2010) Correlated changes in NMDA receptor phosphorylation, functional activity, and sedation by chronic ethanol consumption. Development 115 1112 PMID: 20831600
Vergassola et al (2018) Presynaptic mGlu1 Receptors Control GABAB Receptors in an Antagonist-Like Manner in Mouse Cortical GABAergic and Glutamatergic Nerve Endings. Front Mol Neurosci 11 324 PMID: 30279647
Chacón et al (2012) Focal adhesion kinase regulates actin nucleation and neuronal filopodia formation during axonal growth. J Neurosci 139 3200 PMID: 22872087
Marrocco et al (2012) Anxiety-like behavior of prenatally stressed rats is associated with a selective reduction of glutamate release in the ventral hippocampus. PLoS One 32 17143 PMID: 23197707
Lam et al (2011) Leptin does not directly affect CNS serotonin neurons to influence appetite. J Physiol 13 584 PMID: 21531340
Bragina et al (2015) Differential expression of metabotropic glutamate and GABA receptors at neocortical glutamatergic and GABAergic axon terminals. Front Cell Neurosci 9 345 PMID: 26388733
Lee et al (2015) Modulation of Spinal GABAergic Inhibition and Mechanical Hypersensitivity following Chronic Compression of Dorsal Root Ganglion in the Rat. Neural Plast 2015 924728 PMID: 26451259
Mans et al (2014) An acetylcholinesterase inhibitor, eserine, induces long-term depression at CA3-CA1 synapses in the hippocampus of adult rats. J Neurophysiol 112 2388 PMID: 25143547
Jensen et al (2007) Presynaptic plasma membrane Ca2+ ATPase isoform 2a regulates excitatory synaptic transmission in rat hippocampal CA3. J Neurochem 579 85 PMID: 17170045
Kelm et al (2008) The role of protein kinase A in the ethanol-induced increase in spontaneous GABA release onto cerebellar Purkinje neurons. J Neurophysiol 100 3417 PMID: 18945815
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Reviews for CGP 52432
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Stimulation of epileptiform activity.
By
Sergiy Sylantyev on 12/10/2023
Assay Type: Ex Vivo
Species: Rat
Cell Line/Tissue: Hippocampus
CGP 52432 in high concentration was used to shape epileptiform activity in hippocampal brain tissue. Figure: patterned epileptiform activity (top trace) with synchronized neurotransmitter release (medium trace) from acute hippocampal tissue with high concentration (5 microM) of CGP in perfusion solution.
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