CGP 54626 hydrochloride

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Cat.No. 1088 - CGP 54626 hydrochloride | C18H28Cl2NO3P.HCl | CAS No. 149184-21-4
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% (HPLC)
Datasheet
Citations (33)
Reviews
Literature (6)

Biological Activity

A potent, selective GABAB receptor antagonist (IC50 = 4 nM).

Licensing Information

Sold with the permission of Novartis Pharma AG

Compound Libraries

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

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 Data

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

Preparing Stock Solutions

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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 4.5 mL 22.48 mL 44.97 mL
2.5 mM 0.9 mL 4.5 mL 8.99 mL
5 mM 0.45 mL 2.25 mL 4.5 mL
25 mM 0.09 mL 0.45 mL 0.9 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

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

Brugger et al (1993) The action of new potent GABAB receptor antagonists in the hemisected spinal cord preparation of the rat. Eur.J.Pharmacol. 235 153 PMID: 8390938

Kaupmann et al (1998) GABAB-receptor subtypes assemble into functional heteromeric complexes. Nature 396 683 PMID: 9872317

Froestl et al (1996) Potent, orally active GABAB receptor antagonists. Pharmacol.Rev.Comm. 8 127


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Keywords: CGP 54626 hydrochloride, CGP 54626 hydrochloride supplier, Potent, selective, GABAB, antagonists, Receptors, CGP54626, hydrochloride, 1088, Tocris Bioscience

33 Citations for CGP 54626 hydrochloride

Citations are publications that use Tocris products. Selected citations for CGP 54626 hydrochloride include:

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

Baloucoune et al (2012) GABAB receptor subunit GB1 at the cell surface independently activates ERK1/2 through IGF-1R transactivation. PLoS One 7 e39698 PMID: 22761875

Tani et al (2010) Glutamine is required for persistent epileptiform activity in the disinhibited neocortical brain slice. J Neurosci 30 1288 PMID: 20107056

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

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 24 360 PMID: 28286129

Nagel et al (2015) Synaptic and circuit mechanisms promoting broadband transmission of olfactory stimulus dynamics. Nat Neurosci 18 56 PMID: 25485755

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

Zhang et al (2013) NE drives persistent activity in prefrontal cortex via synergistic α1 and α2 adrenoceptors. PLoS One 8 e66122 PMID: 23785477

Piet et al (2004) Physiological contribution of the astrocytic environment of neurons to intersynaptic crosstalk. Br J Pharmacol 101 2151 PMID: 14766975

Martelli and Fiala (2019) Slow presynaptic mechanisms that mediate adaptation in the olfactory pathway of Drosophila. Elife 8 PMID: 31169499

Scholler (2017) HTS-compatible FRET-based conformational sensors clarify membrane receptor activation. Nat Chem Biol 13 372 PMID: 28135236

Bocchio et al (2015) Increased serotonin transporter expression reduces fear and recruitment of parvalbumin interneurons of the amygdala. Neuropsychopharmacology 40 3015 PMID: 26052039

Lörincz et al (2009) ATP-dependent infra-slow (0.1 Hz) oscillations in thalamic networks. PLoS One 4 e4447 PMID: 19212445

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

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

Pfeffer et al (2013) Inhibition of inhibition in visual cortex: the logic of connections between molecularly distinct interneurons. Nat Neurosci 16 1068 PMID: 23817549

Agarwal and Isacoff (2011) Specializations of a pheromonal glomerulus in the Drosophila olfactory system. J Neurophysiol 105 1711 PMID: 21289134

Dacks et al (2009) Serotonin modulates olfactory processing in the antennal lobe of Drosophila. Nat Neurosci 23 366 PMID: 19863268

Ignell et al (2009) Presynaptic peptidergic modulation of olfactory receptor neurons in Drosophila. Br J Pharmacol 106 13070 PMID: 19625621

Root et al (2008) A presynaptic gain control mechanism fine-tunes olfactory behavior. Neuron 59 311 PMID: 18667158

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

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

Shang et al (2007) Excitatory local circuits and their implications for olfactory processing in the fly antennal lobe. Cell 128 601 PMID: 17289577

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

Tu et al (2010) GABAB receptor activation protects neurons from apoptosis via IGF-1 receptor transactivation. J Neurosci 30 749 PMID: 20071540

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


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