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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.
|Storage||Store at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 429.45. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.2 mM||11.64 mL||58.21 mL||116.43 mL|
|1 mM||2.33 mL||11.64 mL||23.29 mL|
|2 mM||1.16 mL||5.82 mL||11.64 mL|
|10 mM||0.23 mL||1.16 mL||2.33 mL|
References are publications that support the biological activity of the product.
Dolman et al (2007) 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 J.Med.Chem. 50 1558 PMID: 17348638
Dargan et al (2009) ACET is a highly potent and specific kainate receptor antagonist: Characterisation and effects on hippocampal mossy fibre function. Neuropharmacology 56 121 PMID: 18789344
If you know of a relevant reference for ACET, please let us know.
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Keywords: ACET, ACET supplier, Potent, antagonists, GluR5-containing, kainate, receptors, Glutamate, Kainate, Receptors, iGluR, Ionotropic, GluK1, 2728, Tocris Bioscience
2 Citations for ACET
Citations are publications that use Tocris products. Selected citations for ACET include:
Kiyama et al (2019) Essential Roles of Tbr1 in the Formation and Maintenance of the Orientation-Selective J-RGCs and a Group of OFF-Sustained RGCs in Mouse. Cell Rep 27 900 PMID: 30995485
Granger and Nicoll (2014) LTD expression is independent of glutamate receptor subtype. J Virol 6 15 PMID: 25071549
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.
Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.
Learning & Memory Poster
Recognition memory enables us to make judgements about whether or not we have encountered a particular stimulus before. This poster outlines the cellular mechanisms underlying recognition memory and its links to long-term depression, as well as the use of pharmacological intervention to assess the role of neurotransmitters in recognition memory.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.
Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.