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Submit ReviewCGP 46381
Description: Selective GABAB antagonist; brain penetrant
Chemical Name: (3-Aminopropyl)(cyclohexylmethyl)phosphinic acid
Biological Activity for CGP 46381
CGP 46381 is a brain penetrant, selective GABAB receptor antagonist (IC50 = 4.9 μM).
Licensing Information
Sold with the permission of Novartis Pharma AG
Technical Data for CGP 46381
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for CGP 46381
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 21.93 | 100 |
Preparing Stock Solutions for CGP 46381
The following data is based on the product molecular weight 219.26. 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.
| 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 for CGP 46381
References for CGP 46381
References are publications that support the biological activity of the product.
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
Froestl et al (1996) Potent, orally active GABAB receptor antagonists. Pharmacol.Rev.Comm. 8 127
If you know of a relevant reference for CGP 46381, please let us know.
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Keywords: CGP 46381, CGP 46381 supplier, Brain, penetrant, selective, GABAB, antagonist, Receptors, CGP46381, 1247, Tocris Bioscience
5 Citations for CGP 46381
Citations are publications that use Tocris products. Selected citations for CGP 46381 include:
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
Oberlander (2016) 17β-OE Acutely Potentiates Glutamatergic Synaptic Transmission in the Hippocampus through Distinct Mechanisms in Males and Females. J Neurosci 36 2677 PMID: 26937008
Lee and Sherman (2012) Intrinsic modulators of auditory thalamocortical transmission. Hear Res 287 43 PMID: 22726616
Cheng et al (2015) GABAB receptor antagonist CGP46381 inhibits form-deprivation myopia development in guinea pigs. Front Cell Neurosci 2015 207312 PMID: 25649745
Costa et al (2008) Electrophysiology and pharmacology of striatal neuronal dysfunction induced by mitochondrial complex I inhibition. J Neurosci 28 8040 PMID: 18685029
Do you know of a great paper that uses CGP 46381 from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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