Product overview

Name GYKI 53655 hydrochloride
Description Non-competitive AMPA receptor antagonist. Also blocks kainate GluK3 homomeric receptors.
Alternative names LY300168
Purity >98%
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Biological Data

Biological description

Non-competitive AMPA and kainate receptor antagonist. Analog of GYKI 52466.

GYKI 53655 acts via an allosteric site at the AMPAR and inhibits channel gating downstream of glutamate binding.


The compound inhibits AMPA - mediated response in cells expressing human GluR1(GluA1) and GluR4(GluA4) (IC50 values are 6 µM and 5 µM for GluA1 and GluA4 subunits respectively).

At higher concentrations, GYKI 53655 also blocks kainate GluK3 homomeric receptors (IC50 = 63 μM) and GluK2b(R)/GluK3 heteroreceptors (IC50 = 32 μM).


Active in vivo. Shows anticonvulsive and neuroprotective effects.

Solubility & Handling

Storage instructions Room temperature (desiccate)
Solubility overview Soluble in water (100mM, gentle warming) and in DMSO (100 mM)
Important This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.

Calculators

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Dilution

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Chemical Data

Chemical name 1-(4-Aminophenyl)-3-methylcarbamyl- 4-methyl-3,4-dihydro-7,8-methylenedioxy-5H-2,3-benzodiazepine hydrochloride
Molecular Weight 388.85
Chemical structure GYKI 53655  [143692-18-6] Chemical Structure
Molecular Formula C19H20N4O3.HCl
CAS Number 143692-48-2
PubChem identifier 126757
SMILES Cl.Nc1ccc(cc1)C3=NN(C(C)Cc2cc4OCOc4cc23)C(=O)NC
Source Synthetic
InChi InChI=1S/C19H20N4O3.ClH/c1-11-7-13-8-16-17(26-10-25-16)9-15(13)18(22-23(11)19(24)21-2)12-3-5-14(20)6-4-12;/h3-6,8-9,11H,7,10,20H2,1-2H3,(H,21,24);1H
InChiKey ASLCSBBDVWPSQT-UHFFFAOYSA-N
MDL number MFCD01941362
Appearance Orange solid

References for GYKI 53655 hydrochloride

References are publications that support the biological activity of the product
  • 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.
  • Blocking the trigeminal EPSP in rat abducens motoneurons in vivo with the AMPA antagonists NBQX and GYKI 53655.

    Ruiz A et al (2000) Brain Res Bull 52(2) : 99-107.
  • Activity of 2,3-benzodiazepines at native rat and recombinant human glutamate receptors in vitro: stereospecificity and selectivity profiles.

    Bleakman D et al (1996) Neuropharmacology 35(12) : 1689-702.
  • Negative allosteric modulation of wild-type and mutant AMPA receptors by GYKI 53655.

    Partin KM et al (1996) Mol Pharmacol 49(1) : 142-8.