GYKI 52466 dihydrochloride
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. Also available as part of the AMPA Receptor Tocriset™. Also available as part of the Kainate Receptor Tocriset™.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 366.24. 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.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.73 mL||13.65 mL||27.3 mL|
|5 mM||0.55 mL||2.73 mL||5.46 mL|
|10 mM||0.27 mL||1.37 mL||2.73 mL|
|50 mM||0.05 mL||0.27 mL||0.55 mL|
References are publications that support the products' biological activity.
Donevan and Rogawsk (1993) GYKI 52466, a 2,3-benzodiazepine, is a highly selective, non-competitive antagonist of AMPA/kainate receptor responses. Neuron 10 51 PMID: 7678966
Paternain et al (1995) Selective antagonism of AMPA receptors unmasks kainate receptor-mediated responses in hippocampal neurons. Neuron 14 185 PMID: 7826635
Rzeski et al (2001) Glutamate antagonists limit tumor growth. Proc.Natl.Acad.Sci.USA 98 6372 PMID: 11331750
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
Tarnawa et al (1989) Electrophysiological studies with a 2,3-benzodiazepine muscle relaxant: GYKI 52466. Eur.J.Pharmacol. 167 193 PMID: 2574112
If you know of a relevant reference for GYKI 52466 dihydrochloride, please let us know.
View Related Products by Product Action
Keywords: GYKI 52466 dihydrochloride, supplier, Selective, non-competitive, AMPA, antagonists, Glutamate, Receptors, iGlur, Ionotropic, GYKI52466, dihydrochloride, AMPA, Receptors, AMPA, Receptors, Tocris Bioscience
10 Citations for GYKI 52466 dihydrochloride
Citations are publications that use Tocris products. Selected citations for GYKI 52466 dihydrochloride include:
Kopach et al (2011) Inflammation alters trafficking of extrasynaptic AMPA receptors in tonically firing lamina II neurons of the rat spinal dorsal horn. Pain 152 912 PMID: 21282008
Lobb et al (2010) A dynamic role for GABA receptors on the firing pattern of midbrain dopaminergic neurons. J Neurophysiol 104 403 PMID: 20445035
Santos et al (2009) Transmission efficacy and plasticity in glutamatergic synapses formed by excitatory interneurons of the substantia gelatinosa in the rat spinal cord. PLoS One 4 e8047 PMID: 19956641
Fritsch et al (2009) Pathological alterations in GABAergic interneurons and reduced tonic inhibition in the basolateral amygdala during epileptogenesis. Neuroscience 163 415 PMID: 19540312
Lebrun-Julien et al (2009) Excitotoxic death of retinal neurons in vivo occurs via a non-cell-autonomous mechanism. J Neurosci 29 5536 PMID: 19403821
Du et al (2008) The role of hippocampal GluR1 and GluR2 receptors in manic-like behavior. J Neurosci 28 68 PMID: 18171924
Lin et al (2008) Integrin regulation of cytoplasmic calcium in excitatory neurons depends upon glutamate receptors and release from intracellular stores. J Pharmacol Exp Ther 37 770 PMID: 18289871
Huang et al (2004) Astrocyte glutamate transporters regulate metabotropic glutamate receptor-mediated excitation of hippocampal interneurons. J Neurosci 24 4551 PMID: 15140926
Bao et al (2016) Lentinan produces a robust antidepressant-like effect via enhancing the prefrontal Dectin-1/AMPA receptor signaling pathway Behavioural Brain Research 317 263 PMID: 27693847
Fernandes et al (2014) In vitro ischemia triggers a transcriptional response to down-regulate synaptic proteins in hippocampal neurons. PLoS One 9 e99958 PMID: 24960035
Do you know of a great paper that uses GYKI 52466 dihydrochloride from Tocris? If so please let us know.
GYKI 52466 dihydrochloride Reviews
Average Rating:(Based on 0 Reviews)
Literature in this Area
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.
Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.
Learning & Memory Poster
Recognition memory enables us to make judgements about whether or not we have encountered a particular stimulus before. This poster outlines the cellular mechanisms underlying recognition memory and its links to long-term depression, as well as the use of pharmacological intervention to assess the role of neurotransmitters in recognition memory.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.
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.