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. Also available as part of the AMPA Receptor Tocriset™. Also available as part of the Kainate Receptor Tocriset™.
Compound Libraries
GYKI 52466 dihydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 366.24 |
| Formula | C17H15N3O2.2HCl |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 102771-26-6 |
| PubChem ID | 10042240 |
| InChI Key | RUBSCPARMVJNKX-UHFFFAOYSA-N |
| Smiles | Cl.Cl.CC1=NN=C(C2=CC=C(N)C=C2)C2=C(C1)C=C1OCOC1=C2 |
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 | 16.49 | 50 | |
| water | 3.3 | 10 |
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 |
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Product Datasheets
References
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
Keywords: GYKI 52466 dihydrochloride, supplier, Selective, non-competitive, AMPA, antagonists, Glutamate, Receptors, iGlur, Ionotropic, GYKI52466, dihydrochloride, AMPA, Receptors, AMPA, Receptors, Tocris Bioscience
