CGP 54626 hydrochloride
Chemical Name: [S-(R*,R*)]-[3-[[1-(3,4-Dichlorophenyl)ethyl]amino]-2-hydroxypropyl](cyclohexylmethyl) phosphinic acid
Purity: ≥96%
Biological Activity
CGP 54626 hydrochloride is a potent, selective GABAB receptor antagonist (IC50 = 4 nM).Technical Data
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
Background References
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High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
Fox JT, Sakamuru S, Huang R
Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8. -
Probing alpha4betadelta GABAA receptor heterogeneity: differential regional effects of a functionally selective alpha4beta1delta/alpha4beta3delta receptor agonist on tonic and phasic inhibition in rat brain.
Hoestgaard-Jensen K, Dalby N, Krall J, Hammer H, Krogsgaard-Larsen P, Frolund B, Jensen A
J Neurosci, 2014;34(49):16256-72. -
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 -
GABAB-receptor subtypes assemble into functional heteromeric complexes.
Kaupmann et al.
Nature, 1998;396:683 -
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
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Slow presynaptic mechanisms that mediate adaptation in the olfactory pathway of Drosophila.
Authors: Martelli and Fiala
Elife 2019;8
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KCC2 Regulates Neuronal Excitability and Hippocampal Activity via Interaction with Task-3 Channels.
Authors: Goutierre Et al.
Cell Rep 2019;28:91
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Biased OXTergic Modulation of Midbrain DA Systems.
Authors: Xiao Et al.
Neuron 2017;95:368
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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
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FRET-based sensors unravel activation and allosteric modulation of the GABAB receptor.
Authors: Lecat-Guillet
Cell Chem Biol 2017;24(3):360
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HTS-compatible FRET-based conformational sensors clarify membrane receptor activation.
Authors: Scholler
Nat Chem Biol 2017;13(4):372
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Functional integration of a serotonergic neuron in the Drosophila antennal lobe.
Authors: Zhang and Gaudry
Elife 2016;5
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Neuronal splicing regulator RBFOX3(NeuN) regulates adult hippocampal neurogenesis and synaptogenesis
Authors: Lin Et al.
PLoS One 2016;11:e0164164
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Combining two repurposed drugs as a promising approach for Alzheimer's disease therapy.
Authors: Chumakov Et al.
Sci Rep 2015;5:7608
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GABAB receptor upregulates fragile X mental retardation protein expression in neurons.
Authors: Zhang Et al.
Elife 2015;5:10468
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Increased serotonin transporter expression reduces fear and recruitment of parvalbumin interneurons of the amygdala.
Authors: Bocchio Et al.
Neuropsychopharmacology 2015;40:3015
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Morphine disinhibits glutamatergic input to VTA DA neurons and promotes DA neuron excitation.
Authors: Chen Et al.
J Neurosci 2015;4
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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
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Synaptic and circuit mechanisms promoting broadband transmission of olfactory stimulus dynamics.
Authors: Nagel Et al.
Nat Neurosci 2015;18:56
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Modification of Male Courtship Motivation by Olfactory Habituation via the GABAA Receptor in Drosophila melanogaster.
Authors: Tachibana Et al.
PLoS One 2015;10:e0135186
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NE drives persistent activity in prefrontal cortex via synergistic α1 and α2 adrenoceptors.
Authors: Zhang Et al.
PLoS One 2013;8:e66122
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Inhibition of inhibition in visual cortex: the logic of connections between molecularly distinct interneurons.
Authors: Pfeffer Et al.
Nat Neurosci 2013;16:1068
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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
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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
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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
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Specializations of a pheromonal glomerulus in the Drosophila olfactory system.
Authors: Agarwal and Isacoff
J Neurophysiol 2011;105:1711
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GABAB receptor activation protects neurons from apoptosis via IGF-1 receptor transactivation.
Authors: Tu Et al.
J Neurosci 2010;30:749
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Glutamine is required for persistent epileptiform activity in the disinhibited neocortical brain slice.
Authors: Tani Et al.
J Neurosci 2010;30:1288
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ATP-dependent infra-slow (0.1 Hz) oscillations in thalamic networks.
Authors: Lörincz Et al.
PLoS One 2009;4:e4447
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Serotonin modulates olfactory processing in the antennal lobe of Drosophila.
Authors: Dacks Et al.
Nat Neurosci 2009;23:366
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Presynaptic peptidergic modulation of olfactory receptor neurons in Drosophila.
Authors: Ignell Et al.
Br J Pharmacol 2009;106:13070
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A presynaptic gain control mechanism fine-tunes olfactory behavior.
Authors: Root Et al.
Neuron 2008;59:311
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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
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Excitatory local circuits and their implications for olfactory processing in the fly antennal lobe.
Authors: Shang Et al.
Cell 2007;128:601
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GABA regulates dendritic growth by stabilizing lamellipodia in newly generated interneurons of the olfactory bulb.
Authors: Gascon Et al.
J Neurosci 2006;26:12956
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Physiological contribution of the astrocytic environment of neurons to intersynaptic crosstalk.
Authors: Piet Et al.
Br J Pharmacol 2004;101:2151
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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
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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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