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Brain penetrant, selective GABAB receptor antagonist (IC50 = 4.9 μM).
Sold with the permission of Novartis Pharma AG
|Storage||Store at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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 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|
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
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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
Cheng et al (2015) GABAB receptor antagonist CGP46381 inhibits form-deprivation myopia development in guinea pigs. Front Cell Neurosci 2015 207312 PMID: 25649745
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
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* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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.
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.
Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.
Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.