CGP 46381

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Description: Selective GABAB antagonist; brain penetrant
Chemical Name: (3-Aminopropyl)(cyclohexylmethyl)phosphinic acid
Citations (5)
Literature (2)

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

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
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.

Select a batch to recalculate based on the batch molecular weight:
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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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:

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

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

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

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

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.

GABA Receptors Scientific Review

GABA Receptors Scientific Review

Written by Ian Martin, Norman Bowery and Susan Dunn, this review provides a history of the GABA receptor, as well as discussing the structure and function of the various subtypes and the clinical potential of receptor modulators; compounds available from Tocris are listed.

Addiction Poster

Addiction Poster

The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.