CGP 54626 hydrochloride

Name: CGP 54626 hydrochloride
Brand: Tocris Bioscience
SKU: 1088

Tocris Bioscience a Bio-Techne Brand

Catalog # 1088

Citations (33)

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Key Product Details

Description:	Potent and selective GABA_B antagonist
Chemical Name:	[S-(R,R)]-[3-[[1-(3,4-Dichlorophenyl)ethyl]amino]-2-hydroxypropyl](cyclohexylmethyl) phosphinic acid
Purity:	≥96% (HPLC)
Molecular Weight:	444.76

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Biological Activity for CGP 54626 hydrochloride

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

Licensing Information

Sold with the permission of Novartis Pharma AG

Compound Libraries for CGP 54626 hydrochloride

CGP 54626 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for CGP 54626 hydrochloride

M. Wt	444.76
Formula	C₁₈H₂₈Cl₂NO₃P.HCl
Storage	Store at RT
Purity	≥96% (HPLC)
CAS Number	149184-21-4
PubChem ID	197583
InChi Key	ZQCFHOVIXCJPLE-LINSIKMZSA-N
Smiles	OP(CC1CCCCC1)(C[C@@H](O)CN[C@@H](C)C2=CC(Cl)=C(Cl)C=C2)=O.Cl

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.

Solubility for CGP 54626 hydrochloride

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	22.24	50
	ethanol	4.45	10 with gentle warming

Preparing Stock Solutions for CGP 54626 hydrochloride

The following data is based on the product molecular weight 444.76.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.5 mM	4.50 mL	22.48 mL	44.97 mL
2.5 mM	0.90 mL	4.50 mL	8.99 mL
5 mM	0.45 mL	2.25 mL	4.50 mL
25 mM	0.09 mL	0.45 mL	0.90 mL

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References for CGP 54626 hydrochloride

References are publications that support the biological activity of the product.

Kaupmann GABA_B-receptor subtypes assemble into functional heteromeric complexes. Nature 1998 PMID: 9872317
Froestl Potent, orally active GABA_B receptor antagonists. Pharmacol.Rev.Comm.
Brugger The action of new potent GABA_B receptor antagonists in the hemisected spinal cord preparation of the rat. Eur.J.Pharmacol. 1993 PMID: 8390938

Citations for CGP 54626 hydrochloride (33)

Showing 1 - 10 of 33 citations Showing All

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Citations are publications that use Bio-Techne products. Selected citations for CGP 54626 hydrochloride include:

Martelli and Fiala (2019) Slow presynaptic mechanisms that mediate adaptation in the olfactory pathway of Drosophila. Elife. 8
PMID: 31169499
Goutierre et al. (2019) KCC2 Regulates Neuronal Excitability and Hippocampal Activity via Interaction with Task-3 Channels. Cell Rep. 28:91
PMID: 31269453
Lecat-Guillet (2017) FRET-based sensors unravel activation and allosteric modulation of the GABAB receptor. Cell Chem Biol. 24(3):360
PMID: 28286129
Scholler (2017) HTS-compatible FRET-based conformational sensors clarify membrane receptor activation. Nat Chem Biol. 13(4):372
PMID: 28135236
Zhang et al. (2017) Astrocytic Process Plasticity and IKKβ/NF-κB in Central Control of Blood Glucose, Blood Pressure, and Body Weight. Cell Metab. 25:1091
PMID: 28467927
Xiao et al. (2017) Biased OXTergic Modulation of Midbrain DA Systems. Neuron. 95:368
PMID: 28669546
Lin et al. (2016) Neuronal splicing regulator RBFOX3(NeuN) regulates adult hippocampal neurogenesis and synaptogenesis PLoS One. 11:e0164164
PMID: 27701470
Zhang and Gaudry (2016) Functional integration of a serotonergic neuron in the Drosophila antennal lobe. Elife. 5
PMID: 27572257
Bocchio et al. (2015) Increased serotonin transporter expression reduces fear and recruitment of parvalbumin interneurons of the amygdala. Neuropsychopharmacology. 40:3015
PMID: 26052039
Zhang et al. (2015) GABAB receptor upregulates fragile X mental retardation protein expression in neurons. Elife. 5:10468
PMID: 26020477
Chen et al. (2015) Morphine disinhibits glutamatergic input to VTA DA neurons and promotes DA neuron excitation. J Neurosci. 4
PMID: 26208338
Kotecki et al. (2015) GIRK Channels Modulate Opioid-Induced Motor Activity in a Cell Type- and Subunit-Dependent Manner. Proc Natl Acad Sci U S A. 35:7131
PMID: 25948263
Tachibana et al. (2015) Modification of Male Courtship Motivation by Olfactory Habituation via the GABAA Receptor in Drosophila melanogaster. PLoS One. 10:e0135186
PMID: 26252206
Chumakov et al. (2015) Combining two repurposed drugs as a promising approach for Alzheimer's disease therapy. Sci Rep. 5:7608
PMID: 25566747
Nagel et al. (2015) Synaptic and circuit mechanisms promoting broadband transmission of olfactory stimulus dynamics. Nat Neurosci. 18:56
PMID: 25485755
Pfeffer et al. (2013) Inhibition of inhibition in visual cortex: the logic of connections between molecularly distinct interneurons. Nat Neurosci. 16:1068
PMID: 23817549
Zhang et al. (2013) NE drives persistent activity in prefrontal cortex via synergistic α1 and α2 adrenoceptors. PLoS One. 8:e66122
PMID: 23785477
Baloucoune et al. (2012) GABA_B receptor subunit GB1 at the cell surface independently activates ERK1/2 through IGF-1R transactivation. PLoS One. 7:e39698
PMID: 22761875
Werner et al. (2011) PKCγ is required for ethanol-induced increases in GABA(A) receptor α4 subunit expression in cultured cerebral cortical neurons. J Biol Chem. 116:554
PMID: 21155805
Paz et al. (2011) A new mode of corticothalamic transmission revealed in the Gria4(-/-) model of absence epilepsy. Proc Natl Acad Sci U S A. 14:1167
PMID: 21857658
Agarwal and Isacoff (2011) Specializations of a pheromonal glomerulus in the Drosophila olfactory system. J Neurophysiol. 105:1711
PMID: 21289134
Tu et al. (2010) GABA_B receptor activation protects neurons from apoptosis via IGF-1 receptor transactivation. J Neurosci. 30:749
PMID: 20071540
Tani et al. (2010) Glutamine is required for persistent epileptiform activity in the disinhibited neocortical brain slice. J Neurosci. 30:1288
PMID: 20107056
Ignell et al. (2009) Presynaptic peptidergic modulation of olfactory receptor neurons in Drosophila. Br J Pharmacol. 106:13070
PMID: 19625621
Dacks et al. (2009) Serotonin modulates olfactory processing in the antennal lobe of Drosophila. Nat Neurosci. 23:366
PMID: 19863268
Lörincz et al. (2009) ATP-dependent infra-slow (0.1 Hz) oscillations in thalamic networks. PLoS One. 4:e4447
PMID: 19212445
Root et al. (2008) A presynaptic gain control mechanism fine-tunes olfactory behavior. Neuron. 59:311
PMID: 18667158
Binet et al. (2007) Common structural requirements for heptahelical domain function in class A and class C G protein-coupled receptors. J Neurogenet. 282:12154
PMID: 17310064
Shang et al. (2007) Excitatory local circuits and their implications for olfactory processing in the fly antennal lobe. Cell. 128:601
PMID: 17289577
Gascon et al. (2006) GABA regulates dendritic growth by stabilizing lamellipodia in newly generated interneurons of the olfactory bulb. J Neurosci. 26:12956
PMID: 17167085
Piet et al. (2004) Physiological contribution of the astrocytic environment of neurons to intersynaptic crosstalk. Br J Pharmacol. 101:2151
PMID: 14766975
Dzitoyeva et al. (2003) Gamma-aminobutyric acid B receptor 1 mediates behavior-impairing actions of alcohol in Drosophila: adult RNA interference and pharmacological evidence. Proc Natl Acad Sci U S A. 100:5485
PMID: 12692303
Wood et al. (2000) The human GABA(B1b) and GABA(B2) heterodimeric recombinant receptor shows low sensitivity to phaclofen and saclofen. J Neurochem. 131:1050
PMID: 11082110

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