GYKI 52466 Hydrochloride | Ligand-gated Ion Channels | Selective Non-competitive AMPA Antagonist

Category:

Ion Channels

Ligand-gated Ion Channels

Glutamate (Ionotropic) Receptors

AMPA Selective

Antagonists

Cat.No.	Product Name
1454	GYKI 52466 hydrochloride

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GYKI 52466 hydrochloride

Chemical Name: 4-(8-Methyl-9H-1,3-dioxolo[4,5-h][2,3]benzodiazepin-5-y l)-benzenamine hydrochloride

Biological Activity:

Selective non-competitive AMPA receptor antagonist (IC₅₀ values are 10-20, ~ 450 and >> 50 μM for AMPA- , kainate- and NMDA-induced responses respectively). Skeletal muscle relaxant and orally-active anticonvulsant. Has anti-proliferative effects in transformed cells.

Technical Data:

M.Wt:	329.79
Formula:	C₁₇H₁₅N₃O₂.HCl
Storage:	Desiccate at RT
Solubility:	Soluble to 15 mM in 1eq. HCl
Purity:	>99%
CAS No:	[102771-26-6]

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References:

Tarnawa et al (1989) Electrophysiological studies with a 2,3-benzodiazepine muscle relaxant: GYKI 52466. Eur.J.Pharmacol. 167 193. Donevan and Rogawski (1993) GYKI 52466, a 2,3-benzodiazepine, is a highly selective, non-competitive antagonist of AMPA/kainate receptor responses. Neuron 10 51. Paternain et al (1995) Selective antagonism of AMPA receptors unmasks kainate receptor-mediated responses in hippocampal neurons. Neuron 14 185. Rzeski et al (2001) Glutamate antagonists limit tumor growth. Proc.Natl.Acad.Sci.USA 98 6372. 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.

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Keywords: GYKI 52466 Hydrochloride, Ligand-gated Ion Channels, Selective Non-competitive AMPA Antagonist, Tocris Bioscience

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