GYKI 53655 hydrochloride

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Cat.No. 2555 - GYKI 53655 hydrochloride | C19H20N4O3.HCl | CAS No. 143692-48-2
Description: Non-competitive AMPA receptor antagonist
Chemical Name: 1-(4-Aminophenyl)-3-methylcarbamyl-4-methyl-3,4-dihydro-7,8-methylenedioxy-5H-2,3-benzodiazepine hydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations (9)
Literature

Biological Activity

Non-competitive AMPA and kainate receptor antagonist. Analog of GYKI 52466 (Cat. No. 1454). Prolongs the survival time after MgCl2- induced global cerebral ischemia. Exhibits anticonvulsant activity. Also blocks GluK3 homomeric receptors (IC50 = 63 μM) and GluK2b(R)/GluK3 heteroreceptors (IC50 = 32 μM) at high concentrations.

Technical Data

M. Wt 388.85
Formula C19H20N4O3.HCl
Storage Desiccate at RT
Purity ≥99% (HPLC)
CAS Number 143692-48-2
PubChem ID 126757
InChI Key ASLCSBBDVWPSQT-UHFFFAOYSA-N
Smiles CC(N(C(NC)=O)N=C3C4=CC=C(N)C=C4)CC1=C3C=C(OCO2)C2=C1.Cl

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
DMSO 38.88 100
water 38.88 100

Preparing Stock Solutions

The following data is based on the product molecular weight 388.85. 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.57 mL 12.86 mL 25.72 mL
5 mM 0.51 mL 2.57 mL 5.14 mL
10 mM 0.26 mL 1.29 mL 2.57 mL
50 mM 0.05 mL 0.26 mL 0.51 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Paternain et al (1995) Selective antagonism of AMPA receptors unmasks kainate receptor-mediated responses in hippocampal neurons. Neuron 14 185 PMID: 7826635

Szabados et al (2001) Comparison of anticonvulsive and acute neuroprotective activity of three 2,3-benzodiazepine compounds, GYKI 52466, GYKI 53405, and GYKI 53655. Brain Res.Bull. 55 387 PMID: 11489346

Perrais et al (2009) Antagonism of recombinant and native GluK3-containing kainate receptors. Neuropharmacology 56 131 PMID: 18761361


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View all AMPA Receptor Antagonists

Keywords: GYKI 53655 hydrochloride, supplier, GYKI53655, hydrochloride, non-competitive, AMPA, receptors, kainate, antagonists, GluK3, AMPA, Receptors, Tocris Bioscience

9 Citations for GYKI 53655 hydrochloride

Citations are publications that use Tocris products. Selected citations for GYKI 53655 hydrochloride include:

Straub et al (2011) Distinct functions of kainate receptors in the brain are determined by the auxiliary subunit Neto1. Nat Neurosci 14 866 PMID: 21623363

Tang et al (2011) Neto1 is an auxiliary subunit of native synaptic kainate receptors. Cell Rep 31 10009 PMID: 21734292

Biase et al (2010) Excitability and synaptic communication within the oligodendrocyte lineage. J Neurosci 30 3600 PMID: 20219994

Astorga et al (2015) An excitatory GABA loop operating in vivo. Front Cell Neurosci 9 275 PMID: 26236197

Ben-Simon et al (2015) A Combined Optogenetic-Knockdown Strategy Reveals a Major Role of Tomosyn in Mossy Fiber Synaptic Plasticity. PLoS One 12 396 PMID: 26166572

Murphy-Baum and Taylor (2015) The Synaptic and Morphological Basis of Orientation Selectivity in a Polyaxonal Amacrine Cell of the Rabbit Retina. J Neurosci 35 13336 PMID: 26424882

Falgairolle and O'Donovan (2015) Pharmacological Investigation of Fluoro-Gold Entry into Spinal Neurons. Pharmacol Res Perspect 10 e0131430 PMID: 26102354

Höft et al (2014) Heterogeneity in expression of functional ionotropic glutamate and GABA receptors in astrocytes across brain regions: insights from the thalamus. Philos Trans R Soc Lond B Biol Sci 369 20130602 PMID: 25225096

Buldyrev et al (2012) Synaptic pathways that shape the excitatory drive in an OFF retinal ganglion cell. J Neurophysiol 107 1795 PMID: 22205648


Do you know of a great paper that uses GYKI 53655 hydrochloride from Tocris? If so please let us know.

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