GYKI 52466 hydrochloride
(HB0311)
Product overview
| Name | GYKI 52466 hydrochloride |
| Description | Selective, non-competitive AMPA receptor antagonist |
| Alternative names | GYKI-52466 |
| Purity | >98% |
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Biological Data
| Biological description | Selective, non-competitive AMPA receptor antagonist (IC50 values are 10-20, approx. 450 and >50 μM for AMPA- , kainate- and NMDA-induced responses, respectively). Inactive at NMDA receptors. GYKI 52466 shows anti-convulsant and neuroprotective actions. It also acts as a skeletal muscle relaxant. The compounds is active in vivo and its effects have been shown to last from 60 to 90 min with plasma concentrations peaking within 15min and decreasing to <5% of peak levels within 90min of i.p. injection. |
Solubility & Handling
| Storage instructions | room temperature (desiccate) |
| Solubility overview | Soluble in water (10mM) or DMSO (25mM, heating) |
| Important | This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use. |
Chemical Data
| Chemical name | 4-(8-Methyl-9H-1,3-dioxolo[4,5-h][2,3]benzodiazepin-5-yl)-benzenamine hydrochloride |
| Molecular Weight | 329.79 |
| Chemical structure | ![GYKI 52466 [102771-26-6] Chemical Structure](https://hellobio.com/media/catalog/product//h/b/hb0311_2.png "GYKI 52466 [102771-26-6]") |
| Molecular Formula | C17H15N3O2.HCl |
| CAS Number | 102771-26-6 |
| PubChem identifier | 3538 |
| SMILES | CC1=NN=C(C2=CC3=C(C=C2C1)OCO3)C4=CC=C(C=C4)N |
| Source | Synthetic |
| InChi | InChI=1S/C17H15N3O2/c1-10-6-12-7-15-16(22-9-21-15)8-14(12)17(20-19-10)11-2-4-13(18)5-3-11/h2-5,7-8H,6,9,18H2,1H3 |
| InChiKey | LFBZZHVSGAHQPP-UHFFFAOYSA-N |
| MDL number | MFCD00153803 |
| Appearance | Yellow solid |
References for GYKI 52466 hydrochloride
References are publications that support the biological activity of the product
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Pharmacological Preconditioning with GYKI 52466: A Prophylactic Approach to Neuroprotection.
Goulton et al (doi: 10.3389) Front Cell Neurosci. : 54 -
Pharmacological Preconditioning with GYKI 52466: A Prophylactic Approach to Neuroprotection.
Goulton CS et al (2010) Front Neurosci 4 : -
Comparison of anticonvulsive and acute neuroprotective activity of three 2,3-benzodiazepine compounds, GYKI 52466, GYKI 53405, and GYKI 53655.
Szabados T et al (2001) Brain Res Bull 55(3) : 387-91. -
GYKI 52466, a 2,3-benzodiazepine, is a highly selective, noncompetitive antagonist of AMPA/kainate receptor responses.
Donevan SD et al (1993) Neuron 10(1) : 51-9.
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