CGP 54626 hydrochloride

Cat. No. 1088

CGP 54626 hydrochloride C18H28Cl2NO3P.HCl [149184-21-4]

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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).

Licensing Information

Sold with the permission of Novartis Pharma AG

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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

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.

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.

If you know of a relevant reference for this product please let us know.

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

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

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.

Zhang et al (2015) GABAB receptor upregulates fragile X mental retardation protein expression in neurons. Elife 5 10468. PMID: 26020477.

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.

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.

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

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

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.

Do you know of a great paper that uses CGP 54626 hydrochloride from Tocris? If so please let us know.show all ▼show less ▲

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Keywords: CGP 54626 hydrochloride, supplier, Potent, selective, GABAB, antagonists, Receptors, CGP54626, hydrochloride, Tocris Bioscience, GABAB Receptor Antagonist products

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