GYKI 53655 hydrochloride

Cat. No. 2555

GYKI 53655 hydrochloride C19H20N4O3.HCl [143692-48-2]

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Chemical Name: 1-(4-Aminophenyl)-3-methylcarbamyl-4-methyl-3,4-dihydro-7,8-methylenedioxy-5H-2,3-benzodiazepine hydrochloride

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
Solubility:
Soluble to 100 mM in water and to 100 mM in DMSO
Purity:
>99 %
Storage:
Desiccate at RT
CAS No:
143692-48-2

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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

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

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.

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

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

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.

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

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.

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.

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.

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

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

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