GYKI 53655 - CAS 143692-18-6
Category: Inhibitor
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GYKI 53655 is a selective AMPA receptor antagonist with anticonvulsant activity.
Brife Description:
AMPA receptor antagonist
GYKI 53655; GYKI53655; GYKI-53655; 5-(4-aminophenyl)-N,8-dimethyl-8,9-dihydro-[1,3]dioxolo[4,5-h][2,3]benzodiazepine-7-carboxamide
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1.Contributions of AMPA- and kainate-sensitive receptors to the photopic electroretinogram of the Xenopus retina.
Szikra T;Witkovsky P Vis Neurosci. 2001 Mar-Apr;18(2):187-96.
The effects of kainate receptor-preferring glutamate ligands were tested on the electroretinogram (ERG) of the Xenopus retina. Kainate, domoic acid, and 5-iodowillardiine (20-100 microM) acted similarly in every respect. They increased peak amplitudes of the ERG a-, b-, and d-waves significantly over controls. The AMPA-specific antagonist, GYKI 53655, prevented a kainate-induced increase in ERG a- and d-waves, but was without effect on an increase in the b-wave. Once the effect of agonist on the b-wave had peaked, the ERG began to subside, leading to its nearly complete disappearance within 20 min. Prior exposure to GYKI followed by a combination of GYKI + agonist did not significantly slow the rate of b-wave disappearance. Our results indicate that (1) AMPA receptors contribute to ERG a- and d-waves. (2) The kainate-evoked increase in ERG a-, b-, and d-waves probably results, in part, from an excitotoxic swelling of inner retinal processes. (3) The inner retina has a population of GYKI-resistant, kainate-sensitive receptors which may contribute to b-wave generation.
2.Involvement of post-synaptic kainate receptors during synaptic transmission between unitary connections in rat neocortex.
Ali AB Eur J Neurosci. 2003 Jun;17(11):2344-50.
The properties of functional kainate receptor-mediated EPSCs were studied in acute slices from 19-35-day-old rats. EPSCs elicited in pyramidal and fast-spiking cells in layers 2/3 and 5 of the rat motor cortex by extracellular single shock stimulus in the presence of GYKI 53655 and D-2-amino-5-phosphopentanoic resulted in a residual current. This current was not enhanced by cyclothiazide but was blocked by 6-cyano-7-nitroquinoxalin-2,3-dione and is thought to be mediated by kainate receptors. These kainate receptor-mediated currents displayed a wide range of time courses depending on which pre-synaptic fibres were activated. With paired recordings, unitary EPSCs elicited in pyramidal cells were almost totally blocked by GYKI 53655 and D-2-amino-5-phosphopentanoic. However, when L-transpyrrolidine-2,4-dicarboxylate (PDC), a glutamate uptake blocker, was introduced in the bath, the amplitude of kainate receptor-mediated currents, which is resistant to GYKI 53655 and D-2-amino-5-phosphopentanoic, was revealed. The rise and decay time constants of the kainate receptor-mediated currents were identical to control EPSCs. PDC was not required to reveal the kainate receptor-mediated currents elicited in fast-spiking cells which also displayed similar rise and decay time constants to the control EPSCs.
3.Evidence for presynaptically silent synapses in the immature hippocampus.
Yoon JY;Choi S Biochem Biophys Res Commun. 2017 Jan 22;482(4):1375-1380. doi: 10.1016/j.bbrc.2016.12.044. Epub 2016 Dec 8.
Silent synapses show NMDA receptor (NMDAR)-mediated synaptic responses, but not AMPAR-mediated synaptic responses. A prevailing hypothesis states that silent synapses contain NMDARs, but not AMPARs. However, alternative presynaptic hypotheses, according to which AMPARs are present at silent synapses, have been proposed; silent synapses show slow glutamate release via a fusion pore, and glutamate spillover from the neighboring synaptic terminals. Consistent with these presynaptic hypotheses, the peak glutamate concentrations at silent synapses have been estimated to be ≪170 μM, much lower than those seen at functional synapses. Glutamate transients predicted based on the two presynaptic mechanisms have been shown to activate only high-affinity NMDARs, but not low-affinity AMPARs. Interestingly, a previous study has developed a new approach to distinguish between the two presynaptic mechanisms using dextran, an inert macromolecule that reduces the diffusivity of released glutamate: postsynaptic responses through the fusion pore mechanism, but not through the spillover mechanism, are potentiated by reduced glutamate diffusivity. Therefore, we reasoned that if the fusion pore mechanism underlies silent synapses, dextran application would reveal AMPAR-mediated synaptic responses at silent synapses.
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CAS 143692-18-6 GYKI 53655

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