Catalog Number: 1088
Chemical Name: [S-(R*,R*)]-[3-[[1-(3,4-Dichlorophenyl)ethyl]amino]-2-hydroxypropyl](cyclohexylmethyl) phosphinic acid
Biological Activity
A potent, selective GABAB receptor antagonist (IC50 = 4 nM).
Technical Data
  • M.Wt:
    444.76
  • Formula:
    C18H28Cl2NO3P.HCl
  • Solubility:
    Soluble to 50 mM in DMSO and to 10 mM in ethanol with gentle warming
  • Purity:
    >96%
  • Storage:
    Store at RT
  • CAS No:
    149184-21-4
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.
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
Citations:

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

20 Citations: Showing 1 - 10
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  1. FRET-based sensors unravel activation and allosteric modulation of the GABAB receptor.
    Authors: Lecat-Guillet
    Cell Chem Biol 2017;24(3):360
  2. HTS-compatible FRET-based conformational sensors clarify membrane receptor activation.
    Authors: Scholler
    Nat Chem Biol 2017;13(4):372
  3. Neuronal splicing regulator RBFOX3(NeuN) regulates adult hippocampal neurogenesis and synaptogenesis
    Authors: Lin Et al.
    PLoS One 2016;11:e0164164
  4. GABAB receptor upregulates fragile X mental retardation protein expression in neurons.
    Authors: Zhang Et al.
    Elife 2015;5:10468
  5. Increased serotonin transporter expression reduces fear and recruitment of parvalbumin interneurons of the amygdala.
    Authors: Bocchio Et al.
    Neuropsychopharmacology 2015;40:3015
  6. Morphine disinhibits glutamatergic input to VTA dopamine neurons and promotes dopamine neuron excitation.
    Authors: Chen Et al.
    J Neurosci 2015;4
  7. 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
  8. Inhibition of inhibition in visual cortex: the logic of connections between molecularly distinct interneurons.
    Authors: Pfeffer Et al.
    Nat Neurosci 2013;16:1068
  9. 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
  10. 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
  11. 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
  12. GABAB receptor activation protects neurons from apoptosis via IGF-1 receptor transactivation.
    Authors: Tu Et al.
    J Neurosci 2010;30:749
  13. Glutamine is required for persistent epileptiform activity in the disinhibited neocortical brain slice.
    Authors: Tani Et al.
    J Neurosci 2010;30:1288
  14. Serotonin modulates olfactory processing in the antennal lobe of Drosophila.
    Authors: Dacks Et al.
    Nat Neurosci 2009;23:366
  15. Presynaptic peptidergic modulation of olfactory receptor neurons in Drosophila.
    Authors: Ignell Et al.
    Br J Pharmacol 2009;106:13070
  16. A presynaptic gain control mechanism fine-tunes olfactory behavior.
    Authors: Root Et al.
    Neuron 2008;59:311
  17. 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
  18. Physiological contribution of the astrocytic environment of neurons to intersynaptic crosstalk.
    Authors: Piet Et al.
    Br J Pharmacol 2004;101:2151
  19. 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
  20. 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
Expand to show all 20 Citations

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