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CGP 55845 hydrochloride

Cat. No. 1248

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Chemical Name: (2S)-3-[[(1S)-1-(3,4-Dichlorophenyl)ethyl]amino-2-hydroxypropyl](phenylmethyl)phosphinic acid hydrochloride

Biological Activity

Potent, selective GABA_B receptor antagonist (IC₅₀ = 5 nM) that prevents agonist binding (pK_i = 8.35) and inhibits GABA and glutamate release (pEC₅₀ values are 8.08 and 7.85 respectively). Inhibits GABA_B responses to baclofen (IC₅₀ = 130 nM in an isoproterenol assay) and potentiates the hypoglycemic response to glucose in vitro.

Licensing Information

Sold with the permission of Novartis Pharma AG

Technical Data

M.Wt:

438.71

Formula:

C₁₈H₂₂Cl₂NO₃P.HCl

Solubility:

Soluble to 100 mM in DMSO with gentle warming

Purity:

>98 %

Storage:

Store at RT

CAS No:

149184-22-5

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Resources

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch

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Safety Data Sheet: View Safety Data Sheet

References

Waldmeier et al (1994) GABA and glutamate release affected by GABA_B receptor antagonists with similar potency: no evidence for pharmacologically different presynaptic receptors. Br.J.Pharmacol. 113 1515. PMID: 7889310.

Cunninghan and Enna (1996) Evidence for pharmacologically distinct GABA_B receptors associated with cAMP production in rat brain. Brain Res. 720 220. PMID: 8782915.

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

Deisz (1999) The GABA_B antagonist CGP 55845A reduces presynaptic GABA₁ actions in neurons of the rat in vitro. Neuroscience 93 1241. PMID: 10501448.

Zhang et al (2007) Neurotransmitter mechanisms mediating low-glucose signalling in cocultures and fresh tissue slices of rat carotid body. J.Physiol. 578 735. PMID: 17124268.

Salah and Perkins (2008) Effects of subtype-selective group I mGluR antagonists on synchronous activity induced by 4-aminopyridine/CGP 55845 in adult guinea pig hippocampal slices. Neuropharmacology 55 47. PMID: 18538357.

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