CGP 52432

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Description: Potent and selective GABAB antagonist
Chemical Name: 3-[[(3,4-Dichlorophenyl)methyl]amino]propyl] diethoxymethyl)phosphinic acid
Purity: ≥98% (HPLC)
Datasheet
Citations (22)
Reviews (1)
Literature (2)

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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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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


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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:

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

Lam et al (2011) Leptin does not directly affect CNS serotonin neurons to influence appetite. J Physiol 13 584 PMID: 21531340

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

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

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

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

Moore et al (2009) Plasticity of burst firing induced by synergistic activation of metabotropic glutamate and acetylcholine receptors. Neuron 61 287 PMID: 19186170

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

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

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

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

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

Wu et al (2010) Correlated changes in NMDA receptor phosphorylation, functional activity, and sedation by chronic ethanol consumption. Development 115 1112 PMID: 20831600

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


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Reviews for CGP 52432

Average Rating: 4 (Based on 1 Review.)

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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.

PMID: 36921605
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Literature in this Area

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