CGP 52432

Pricing Availability Delivery Time Qty
Cat.No. 1246 - CGP 52432 | C15H24Cl2NO4P | CAS No. 139667-74-6
Description: Potent, selective GABAB antagonist
Chemical Name: 3-[[(3,4-Dichlorophenyl)methyl]amino]propyl] diethoxymethyl)phosphinic acid
Purity: ≥98% (HPLC)
Datasheet
Citations (16)
Literature

Biological Activity

Potent, selective GABAB receptor antagonist (IC50 = 85 nM).

Licensing Information

Sold with the permission of Novartis Pharma AG

Technical Data

M. Wt 384.24
Formula C15H24Cl2NO4P
Storage Desiccate 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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 3.84 10mM with sonication

Preparing Stock Solutions

The following data is based on the product molecular weight 384.24. Batch specific molecular weights may vary from batch to batch due to solvent 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
1 mM 2.6 mL 13.01 mL 26.03 mL
5 mM 0.52 mL 2.6 mL 5.21 mL
10 mM 0.26 mL 1.3 mL 2.6 mL
50 mM 0.05 mL 0.26 mL 0.52 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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 PMID:


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Keywords: CGP 52432, supplier, Potent, selective, GABAB, antagonists, Receptors, CGP52432, GABAB, Receptors, GABAB, Receptors, Tocris Bioscience

16 Citations for CGP 52432

Citations are publications that use Tocris products. Selected citations for CGP 52432 include:

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

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

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

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

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

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

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

Parker et al (2011) Attenuating GABA(A) receptor signaling in dopamine neurons selectively enhances reward learning and alters risk preference in mice. J Neurosci 31 17103 PMID: 22114279

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

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

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

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


Do you know of a great paper that uses CGP 52432 from Tocris? If so please let us know.

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