GYKI 52466 dihydrochloride

Catalog # Availability Size / Price Qty
GYKI 52466 dihydrochloride | CAS No. 2319722-40-0 | AMPA Receptor Antagonists
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Description: Selective non-competitive AMPA antagonist

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

Purity: ≥98%

Product Details
Citations (18)
Supplemental Products
Reviews (1)

Biological Activity

GYKI 52466 dihydrochloride is a selective noncompetitive 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

Soluble to 50 mM in DMSO and to 10 mM in water
Store at -20°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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Citations for GYKI 52466 dihydrochloride

The citations listed below are publications that use Tocris products. Selected citations for GYKI 52466 dihydrochloride include:

18 Citations: Showing 1 - 10

  1. Pharmacological characterisation of S 47445, a novel positive allosteric modulator of AMPA receptors.
    Authors: Bretin Et al.
    PLoS One  2017;12:e0184429
  2. The Prefrontal Dectin-1/AMPA Receptor Signaling Pathway Mediates The Robust and Prolonged Antidepressant Effect of Proteo-β-Glucan from Maitake.
    Authors: Bao Et al.
    Sci Rep  2016;6:28395
  3. Lentinan produces a robust antidepressant-like effect via enhancing the prefrontal Dectin-1/AMPA receptor signaling pathway
    Authors: Bao Et al.
    Behavioural Brain Research  2016;317:263
  4. 3'-Deoxyadenosine (Cordycepin) Produces a Rapid and Robust Antidepressant Effect via Enhancing Prefrontal AMPA Receptor Signaling Pathway.
    Authors: Li Et al.
    Int J Neuropsychopharmacol  2016;19
  5. In vitro ischemia triggers a transcriptional response to down-regulate synaptic proteins in hippocampal neurons.
    Authors: Fernandes Et al.
    PLoS One  2014;9:e99958
  6. Nitric oxide modulates the temporal properties of the glutamate response in type 4 OFF bipolar cells.
    Authors: Vielma Et al.
    PLoS One  2014;9:e114330
  7. Inflammation alters trafficking of extrasynaptic AMPA receptors in tonically firing lamina II neurons of the rat spinal dorsal horn.
    Authors: Kopach Et al.
    Pain  2011;152:912
  8. Antidepressant-like effects of an AMPA receptor potentiator under a chronic mild stress paradigm.
    Authors: Farley Et al.
    Int J Neuropsychopharmacol  2010;13:1207
  9. A dynamic role for GABA receptors on the firing pattern of midbrain DArgic neurons.
    Authors: Lobb Et al.
    J Neurophysiol  2010;104:403
  10. Transmission efficacy and plasticity in glutamatergic synapses formed by excitatory interneurons of the substantia gelatinosa in the rat spinal cord.
    Authors: Santos Et al.
    PLoS One  2009;4:e8047


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Great results using GYKI in electrophysiology experiments
By Anonymous on 08/21/2018

We use GYKI 52466 dihydrochloride at 10uM to inhibit AMPA receptors during our electrophysiology experiments. This allows us to isolate and study the effects of manipulations on other glutamate receptors. In the set of experiments we used this product for we were examining Kainate receptor properties and so the GYKI was used in conjunction with an NMDAR antagonist.

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