CGP 52432

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1246/50
CGP 52432 | CAS No. 139667-74-6 | GABA-B Receptor Antagonists
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Description: Potent and selective GABAB antagonist

Chemical Name: 3-[[(3,4-Dichlorophenyl)methyl]amino]propyl] diethoxymethyl)phosphinic acid

Purity: ≥98%

Product Details
Citations (22)
Supplemental Products
Reviews

Biological Activity

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

Technical Data

M.Wt:
384.24
Formula:
C15H24Cl2NO4P
Solubility:
Soluble to 10 mM in water with sonication
Purity:
≥98%
Storage:
Desiccate at +4°C
CAS No:
139667-74-6

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.

Additional Information

Licensing Caveats:
Sold with the permission of Novartis Pharma AG

Background References

  1. GABAB receptors as potential targets for drugs able to prevent excessive excitatory amino acid transmission in the spinal cord.
    Bonanno et al.
    Eur.J.Pharmacol., 1998;362:143
  2. Blockade of GABAB receptors facilitates muscarinic agonist-induced epileptiform activity in immature rat piriform cortex in vitro.
    Libri et al.
    Naunyn Schmiedebergs Arch.Pharmacol., 1998;358:168
  3. CGP 52432: a novel potent and selective GABAB autoreceptor antagonist in rat cerebral cortex.
    Lanza et al.
    Eur.J.Pharmacol., 1993;237:191
  4. Potent, orally active GABAB receptor antagonists.
    Froestl et al.
    Pharmacol.Rev.Comm., 1996;8:127

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Citations for CGP 52432

The citations listed below are publications that use Tocris products. Selected citations for CGP 52432 include:

22 Citations: Showing 1 - 10

  1. Presynaptic mGlu1 Receptors Control GABAB Receptors in an Antagonist-Like Manner in Mouse Cortical GABAergic and Glutamatergic Nerve Endings.
    Authors: Vergassola Et al.
    Front Mol Neurosci  2018;11:324
  2. Chronic social isolation reduces 5-HT neuronal activity via upregulated SK3 calcium-activated potassium channels
    Authors: Sargin Et al.
    Elife  2016;5:e21416
  3. Vasculo-neuronal coupling: retrograde vascular communication to brain neurons
    Authors: Jung Kim Et al.
    The Journal of Neuroscience  2016;14:12624
  4. Differential expression of metabotropic glutamate and GABA receptors at neocortical glutamatergic and GABAergic axon terminals.
    Authors: Bragina Et al.
    Front Cell Neurosci  2015;9:345
  5. Modulation of Spinal GABAergic Inhibition and Mechanical Hypersensitivity following Chronic Compression of Dorsal Root Ganglion in the Rat.
    Authors: Lee Et al.
    Neural Plast  2015;2015:924728
  6. Caffeine Modulates Vesicle Release and Recovery at Cerebellar Parallel Fibre Terminals, Independently of Calcium and Cyclic AMP Signalling.
    Authors: Dobson Et al.
    J Pharmacol Exp Ther  2015;10:e0125974
  7. An acetylcholinesterase inhibitor, eserine, induces long-term depression at CA3-CA1 synapses in the hippocampus of adult rats.
    Authors: Mans Et al.
    J Neurophysiol  2014;112:2388
  8. Different transporter systems regulate extracellular GABA from vesicular and non-vesicular sources.
    Authors: Song Et al.
    Front Cell Neurosci  2013;7:23
  9. PropF. inhibits superoxide production, elastase release, and chemotaxis in formyl peptide-activated human neutrophils by blocking formyl peptide receptor 1.
    Authors: Yang Et al.
    J Immunol  2013;190:6511
  10. Postnatal development of synaptic properties of the GABAergic projection from the inferior colliculus to the auditory thalamus.
    Authors: Venkataraman and Bartlett
    J Neurophysiol  2013;109:2866
  11. The role of inhibition in oscillatory wave dynamics in the cortex.
    Authors: Xiao Et al.
    Eur J Neurosci  2012;36:2201
  12. Anxiety-like behavior of prenatally stressed rats is associated with a selective reduction of glutamate release in the ventral hippocampus.
    Authors: Marrocco Et al.
    PLoS One  2012;32:17143
  13. Developmental regulation of CB1-mediated spike-time dependent depression at immature mossy fiber-CA3 synapses.
    Authors: Caiati Et al.
    Sci Rep  2012;2:285
  14. Focal adhesion kinase regulates actin nucleation and neuronal filopodia formation during axonal growth.
    Authors: Chacón Et al.
    J Neurosci  2012;139:3200
  15. Synergistic activation of DA D1 and TrkB receptors mediate gain control of synaptic plasticity in the basolateral amygdala.
    Authors: Li Et al.
    PLoS One  2011;6:e26065
  16. Attenuating GABA(A) receptor signaling in DA neurons selectively enhances reward learning and alters risk preference in mice.
    Authors: Parker Et al.
    J Neurosci  2011;31:17103
  17. Leptin does not directly affect CNS serotonin neurons to influence appetite.
    Authors: Lam Et al.
    J Physiol  2011;13:584
  18. Endogenous N-acetylaspartylglutamate (NAAG) inhibits synaptic plasticity/transmission in the amygdala in a mouse inflammatory pain model.
    Authors: Adedoyin Et al.
    Mol Pain  2010;6:60
  19. Correlated changes in NMDA receptor phosphorylation, functional activity, and sedation by chronic ethanol consumption.
    Authors: Wu Et al.
    Development  2010;115:1112
  20. Plasticity of burst firing induced by synergistic activation of metabotropic glutamate and acetylcholine receptors.
    Authors: Moore Et al.
    Neuron  2009;61:287
  21. The role of protein kinase A in the ethanol-induced increase in spontaneous GABA release onto cerebellar Purkinje neurons.
    Authors: Kelm Et al.
    J Neurophysiol  2008;100:3417
  22. Presynaptic plasma membrane Ca2+ ATPase isoform 2a regulates excitatory synaptic transmission in rat hippocampal CA3.
    Authors: Jensen Et al.
    J Neurochem  2007;579:85

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