GYKI 52466, Selective non-competitive AMPA antagonist (ab120336)
Key features and details
- Selective non-competitive AMPA antagonist
- CAS Number: 102771-26-6
- Soluble in 1eq. HCl to 10mM and in DMSO to 25 mM (with heating)
- Form / State: Solid
- Source: Synthetic
Overview
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Product name
GYKI 52466, Selective non-competitive AMPA antagonist -
Description
Selective non-competitive AMPA antagonist -
Biological description
Selective non-competitive AMPA receptor antagonist (IC50 values are 10-20, approx. 450 and >50 μM for AMPA- , kainate- and NMDA-induced responses, respectively). Skeletal muscle relaxant, orally active anticonvulsant, neuroprotective and anxiolytic in vivo.
Also available in simple stock solutions (ab146716) - add 1 ml of water to get an exact, ready-to-use concentration. -
CAS Number
102771-26-6 -
Chemical structure
Properties
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Chemical name
4-(8-Methyl-9H-1,3-dioxolo[4,5-h][2,3]benzodiazepin-5-yl)-benzenamine hydrochloride -
Molecular weight
329.79 -
Molecular formula
C17H15N3O2.HCl -
PubChem identifier
10042240 -
Storage instructions
Store at Room Temperature. Store under desiccating conditions. The product can be stored for up to 12 months. -
Solubility overview
Soluble in 1eq. HCl to 10mM and in DMSO to 25 mM (with heating) -
Handling
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Refer to SDS for further information
Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
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SMILES
Cl.Nc1ccc(cc1)C3=NN=C(C)Cc2cc4OCOc4cc23 -
Source
Synthetic
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Research areas
Applications
The Abpromise guarantee
Our Abpromise guarantee covers the use of ab120336 in the following tested applications.
The application notes include recommended starting dilutions; optimal dilutions/concentrations should be determined by the end user.
| Application | Abreviews | Notes |
|---|---|---|
| Functional Studies |
Use at an assay dependent concentration.
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| Notes |
|---|
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Functional Studies
Use at an assay dependent concentration. |
Images
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Chemical Structure - GYKI 52466, Selective non-competitive AMPA antagonist (ab120336)2D chemical structure image of ab120336, GYKI 52466, Selective non-competitive AMPA antagonist
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Functional Studies - GYKI 52466, Selective non-competitive AMPA antagonist (ab120336)ab96379 staining MEK1 (phospho S298) in SK-N-SH cells treated with GYKI 52466 (ab120336), by ICC/IF. Decrease in MEK1 (phospho S298) expression correlates with increased concentration of GYKI 52466, as described in literature.
The cells were incubated at 37°C for 1h in media containing different concentrations of ab120336 (GYKI 52466) in DMSO, fixed with 4% formaldehyde for 10 minutes at room temperature and blocked with PBS containing 10% goat serum, 0.3 M glycine, 1% BSA and 0.1% tween for 2h at room temperature. Staining of the treated cells with ab96379 (1/100 dilution) was performed overnight at 4°C in PBS containing 1% BSA and 0.1% tween. A DyLight 488 goat anti-rabbit polyclonal antibody (ab96899) at 1/250 dilution was used as the secondary antibody.
Protocols
To our knowledge, customised protocols are not required for this product. Please try the standard protocols listed below and let us know how you get on.
References (6)
ab120336 has been referenced in 6 publications.
- Srivastava R et al. Cocaine-taking and cocaine-seeking behaviors in rats remain stable after systemic administration of GYKI 52466: a non-competitive AMPA receptor antagonist. Neurosci Lett 508:106-9 (2012). PubMed: 22206835
- Platt NJ et al. Striatal dopamine transmission is subtly modified in human A53Ta-synuclein overexpressing mice. PLoS One 7:e36397 (2012). PubMed: 22570709
- Threlfell S et al. Striatal dopamine release is triggered by synchronized activity in cholinergic interneurons. Neuron 75:58-64 (2012). PubMed: 22794260
- Sasaki T et al. Application of an optogenetic byway for perturbing neuronal activity via glial photostimulation. Proc Natl Acad Sci U S A 109:20720-5 (2012). PubMed: 23185019
- Hartung H et al. Nitric oxide donors enhance the frequency dependence of dopamine release in nucleus accumbens. Neuropsychopharmacology 36:1811-22 (2011). PubMed: 21508928
- Threlfell S et al. Striatal muscarinic receptors promote activity dependence of dopamine transmission via distinct receptor subtypes on cholinergic interneurons in ventral versus dorsal striatum. J Neurosci 30:3398-408 (2010). PubMed: 20203199