CGP 54626 hydrochloride

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Cat.No. 1088 - CGP 54626 hydrochloride | C18H28Cl2NO3P.HCl | CAS No. 149184-21-4
Description: Potent, 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 (19)

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 Plus. 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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 22.24 50
ethanol 4.45 10mM 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 solvent 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
1 mM 2.25 mL 11.24 mL 22.48 mL
5 mM 0.45 mL 2.25 mL 4.5 mL
10 mM 0.22 mL 1.12 mL 2.25 mL
50 mM 0.04 mL 0.22 mL 0.45 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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 PMID:


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Keywords: Potent selective GABAB antagonists Receptors CGP54626 hydrochloride GABAB Receptors

19 Citations for CGP 54626 hydrochloride

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

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

Tu et al (2010) GABAB 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

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

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

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

Lecat-Guillet (2017) FRET-based sensors unravel activation and allosteric modulation of the GABAB receptor. Cell Chem Biol 24 360 PMID: 28286129

Lin et al (2016) Neuronal splicing regulator RBFOX3(NeuN) regulates adult hippocampal neurogenesis and synaptogenesis PLoS One 11 e0164164 PMID: 27701470

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 dopamine neurons and promotes dopamine 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

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

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

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


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