CGP 54626 hydrochloride

Catalog # Availability Size / Price Qty
CGP 54626 hydrochloride | CAS No. 149184-21-4 | GABA-B Receptor Antagonists
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Description: Potent and selective GABAB antagonist

Chemical Name: [S-(R*,R*)]-[3-[[1-(3,4-Dichlorophenyl)ethyl]amino]-2-hydroxypropyl](cyclohexylmethyl) phosphinic acid

Purity: ≥96%

Product Details
Citations (33)
Supplemental Products

Biological Activity

CGP 54626 hydrochloride is a potent, selective GABAB receptor antagonist (IC50 = 4 nM).

Technical Data

Soluble to 50 mM in DMSO and to 10 mM in ethanol with gentle warming
Store at RT

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. The action of new potent GABAB receptor antagonists in the hemisected spinal cord preparation of the rat.
    Brugger et al.
    Eur.J.Pharmacol., 1993;235:153
  2. GABAB-receptor subtypes assemble into functional heteromeric complexes.
    Kaupmann et al.
    Nature, 1998;396:683
  3. Potent, orally active GABAB receptor antagonists.
    Froestl et al.
    Pharmacol.Rev.Comm., 1996;8:127

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Citations for CGP 54626 hydrochloride

The citations listed below are publications that use Tocris products. Selected citations for CGP 54626 hydrochloride include:

33 Citations: Showing 1 - 10

  1. Slow presynaptic mechanisms that mediate adaptation in the olfactory pathway of Drosophila.
    Authors: Martelli and Fiala
    Elife  2019;8
  2. KCC2 Regulates Neuronal Excitability and Hippocampal Activity via Interaction with Task-3 Channels.
    Authors: Goutierre Et al.
    Cell Rep  2019;28:91
  3. Biased OXTergic Modulation of Midbrain DA Systems.
    Authors: Xiao Et al.
    Neuron  2017;95:368
  4. Astrocytic Process Plasticity and IKKβ/NF-κB in Central Control of Blood Glucose, Blood Pressure, and Body Weight.
    Authors: Zhang Et al.
    Cell Metab  2017;25:1091
  5. FRET-based sensors unravel activation and allosteric modulation of the GABAB receptor.
    Authors: Lecat-Guillet
    Cell Chem Biol  2017;24(3):360
  6. HTS-compatible FRET-based conformational sensors clarify membrane receptor activation.
    Authors: Scholler
    Nat Chem Biol  2017;13(4):372
  7. Functional integration of a serotonergic neuron in the Drosophila antennal lobe.
    Authors: Zhang and Gaudry
    Elife  2016;5
  8. Neuronal splicing regulator RBFOX3(NeuN) regulates adult hippocampal neurogenesis and synaptogenesis
    Authors: Lin Et al.
    PLoS One  2016;11:e0164164
  9. Combining two repurposed drugs as a promising approach for Alzheimer's disease therapy.
    Authors: Chumakov Et al.
    Sci Rep  2015;5:7608
  10. GABAB receptor upregulates fragile X mental retardation protein expression in neurons.
    Authors: Zhang Et al.
    Elife  2015;5:10468
  11. Increased serotonin transporter expression reduces fear and recruitment of parvalbumin interneurons of the amygdala.
    Authors: Bocchio Et al.
    Neuropsychopharmacology  2015;40:3015
  12. Morphine disinhibits glutamatergic input to VTA DA neurons and promotes DA neuron excitation.
    Authors: Chen Et al.
    J Neurosci  2015;4
  13. GIRK Channels Modulate Opioid-Induced Motor Activity in a Cell Type- and Subunit-Dependent Manner.
    Authors: Kotecki Et al.
    Proc Natl Acad Sci U S A  2015;35:7131
  14. Synaptic and circuit mechanisms promoting broadband transmission of olfactory stimulus dynamics.
    Authors: Nagel Et al.
    Nat Neurosci  2015;18:56
  15. Modification of Male Courtship Motivation by Olfactory Habituation via the GABAA Receptor in Drosophila melanogaster.
    Authors: Tachibana Et al.
    PLoS One  2015;10:e0135186
  16. NE drives persistent activity in prefrontal cortex via synergistic α1 and α2 adrenoceptors.
    Authors: Zhang Et al.
    PLoS One  2013;8:e66122
  17. Inhibition of inhibition in visual cortex: the logic of connections between molecularly distinct interneurons.
    Authors: Pfeffer Et al.
    Nat Neurosci  2013;16:1068
  18. GABAB receptor subunit GB1 at the cell surface independently activates ERK1/2 through IGF-1R transactivation.
    Authors: Baloucoune Et al.
    PLoS One  2012;7:e39698
  19. A new mode of corticothalamic transmission revealed in the Gria4(-/-) model of absence epilepsy.
    Authors: Paz Et al.
    Proc Natl Acad Sci U S A  2011;14:1167
  20. PKCγ is required for ethanol-induced increases in GABA(A) receptor α4 subunit expression in cultured cerebral cortical neurons.
    Authors: Werner Et al.
    J Biol Chem  2011;116:554
  21. Specializations of a pheromonal glomerulus in the Drosophila olfactory system.
    Authors: Agarwal and Isacoff
    J Neurophysiol  2011;105:1711
  22. GABAB receptor activation protects neurons from apoptosis via IGF-1 receptor transactivation.
    Authors: Tu Et al.
    J Neurosci  2010;30:749
  23. Glutamine is required for persistent epileptiform activity in the disinhibited neocortical brain slice.
    Authors: Tani Et al.
    J Neurosci  2010;30:1288
  24. ATP-dependent infra-slow (0.1 Hz) oscillations in thalamic networks.
    Authors: Lörincz Et al.
    PLoS One  2009;4:e4447
  25. Serotonin modulates olfactory processing in the antennal lobe of Drosophila.
    Authors: Dacks Et al.
    Nat Neurosci  2009;23:366
  26. Presynaptic peptidergic modulation of olfactory receptor neurons in Drosophila.
    Authors: Ignell Et al.
    Br J Pharmacol  2009;106:13070
  27. A presynaptic gain control mechanism fine-tunes olfactory behavior.
    Authors: Root Et al.
    Neuron  2008;59:311
  28. Common structural requirements for heptahelical domain function in class A and class C G protein-coupled receptors.
    Authors: Binet Et al.
    J Neurogenet  2007;282:12154
  29. Excitatory local circuits and their implications for olfactory processing in the fly antennal lobe.
    Authors: Shang Et al.
    Cell  2007;128:601
  30. GABA regulates dendritic growth by stabilizing lamellipodia in newly generated interneurons of the olfactory bulb.
    Authors: Gascon Et al.
    J Neurosci  2006;26:12956
  31. Physiological contribution of the astrocytic environment of neurons to intersynaptic crosstalk.
    Authors: Piet Et al.
    Br J Pharmacol  2004;101:2151
  32. Gamma-aminobutyric acid B receptor 1 mediates behavior-impairing actions of alcohol in Drosophila: adult RNA interference and pharmacological evidence.
    Authors: Dzitoyeva Et al.
    Proc Natl Acad Sci U S A  2003;100:5485
  33. The human GABA(B1b) and GABA(B2) heterodimeric recombinant receptor shows low sensitivity to phaclofen and saclofen.
    Authors: Wood Et al.
    J Neurochem  2000;131:1050


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