CGP 46381

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Cat.No. 1247 - CGP 46381 | C10H22NO2P | CAS No. 123691-14-5
Description: Brain penetrant, selective GABAB antagonist
Chemical Name: (3-Aminopropyl)(cyclohexylmethyl)phosphinic acid
Datasheet
Citations (4)
Literature

Biological Activity

Brain penetrant, selective GABAB receptor antagonist (IC50 = 4.9 μM).

Licensing Information

Sold with the permission of Novartis Pharma AG

Technical Data

M. Wt 219.26
Formula C10H22NO2P
Storage Store at RT
CAS Number 123691-14-5
PubChem ID 130022
InChI Key XOESDNIUAWGCLU-UHFFFAOYSA-N
Smiles NCCCP(CC1CCCCC1)(O)=O

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
water 21.93 100

Preparing Stock Solutions

The following data is based on the product molecular weight 219.26. 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.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 4.56 mL 22.8 mL 45.61 mL
5 mM 0.91 mL 4.56 mL 9.12 mL
10 mM 0.46 mL 2.28 mL 4.56 mL
50 mM 0.09 mL 0.46 mL 0.91 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Curtis and Lacey (1998) Prolonged GABAB receptor-mediated synaptic inhibition in the cat spinal cord: an in vivo study. Exp.Brain Res. 121 319 PMID: 9746138

Staubli et al (1999) GABAB receptor antagonism: facilitatory effects on memory parallel those on LTP induced by TBS but not HFS. J.Neurosci. 19 4609 PMID: 10341258

Lingenhoehl and Olpe (1993) Blockade of the late inhibitory postsynaptic potential in vivo by the GABAB antagonist CGP 46381. Pharmacol.Comm. 3 49 PMID:

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


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Keywords: CGP 46381, supplier, Brain, penetrant, selective, GABAB, antagonist, Receptors, CGP46381, GABAB, Receptors, GABAB, Receptors, Tocris Bioscience

4 Citations for CGP 46381

Citations are publications that use Tocris products. Selected citations for CGP 46381 include:

Lee and Sherman (2012) Intrinsic modulators of auditory thalamocortical transmission. Hear Res 287 43 PMID: 22726616

Pacey et al (2011) Subchronic administration and combination metabotropic glutamate and GABAB receptor drug therapy in fragile X syndrome. Biomed Res Int 338 897 PMID: 21636656

Costa et al (2008) Electrophysiology and pharmacology of striatal neuronal dysfunction induced by mitochondrial complex I inhibition. J Neurosci 28 8040 PMID: 18685029

Cheng et al (2015) GABAB receptor antagonist CGP46381 inhibits form-deprivation myopia development in guinea pigs. Front Cell Neurosci 2015 207312 PMID: 25649745


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