ACET
Chemical Name: (S)-1-(2-Amino-2-carboxyethyl)-3-(2-carboxy-5-phenylthiophene-3-yl-methyl)-5-methylpyrimidine-2,4-dione
Purity: ≥98%
Biological Activity
ACET is a potent and selective GluK1 (formerly GluR5) containing kainate receptor antagonist (IC50 = 7 nM) that displays selectivity over GluK2 (formerly GluR6) containing kainate, NMDA, AMPA and group I mGlu receptors. Reversibly blocks induction of NMDA receptor-independent long term potentiation (LTP) in vitro at nanomolar concentrations.Please refer to IUPHAR Guide to Pharmacology for the most recent naming conventions.
Technical Data
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.
Background References
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Differential signalling and glutamate receptor compositions in the OFF bipolar cell types in the mouse retina
T Ichinose, CB Hellmer
J. Physiol. (Lond.), 2016;594(4):883-94. -
Activity-dependent upregulation of presynaptic kainate receptors at immature CA3-CA1 synapses.
Clarke V, Molchanova S, Hirvonen T, Taira T, Lauri S
J Neurosci, 2014;34(50):16902-16. -
ACET is a highly potent and specific kainate receptor antagonist: Characterisation and effects on hippocampal mossy fibre function.
Dargan et al.
Neuropharmacology, 2009;56:121 -
Synthesis and pharmacological characterisation of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonis
Dolman et al.
J.Med.Chem., 2007;50:1558
Product Datasheets
Citations for ACET
The citations listed below are publications that use Tocris products. Selected citations for ACET include:
2 Citations: Showing 1 - 2
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Essential Roles of Tbr1 in the Formation and Maintenance of the Orientation-Selective J-RGCs and a Group of OFF-Sustained RGCs in Mouse.
Authors: Kiyama Et al.
Cell Rep 2019;27:900
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LTD expression is independent of glutamate receptor subtype.
Authors: Granger and Nicoll
J Virol 2014;6:15
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