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Positive allosteric modulator of AMPA receptors that potently inhibits AMPA receptor desensitization. Selective for the flip variant of each of the four receptor subunits.
|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 389.87. 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|
|1 mM||2.56 mL||12.82 mL||25.65 mL|
|5 mM||0.51 mL||2.56 mL||5.13 mL|
|10 mM||0.26 mL||1.28 mL||2.56 mL|
|50 mM||0.05 mL||0.26 mL||0.51 mL|
References are publications that support the biological activity of the product.
Desai et al (1995) Cyclothiazide acts at a site on the α-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid receptor complex that does not recognise competitive or noncompetitive AMPA receptor antagonists. J.Pharmacol.Exp.Ther. 272 38 PMID: 7529311
Donevan and Rogawski (1998) Allosteric regulation of a-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid receptors by thiocyanate and cyclothiazide at a common modulatory site distinct from that of 2,3-benzodiazepines. Neuroscience 87 615 PMID: 9758228
Kessler et al (2000) The norbornenyl moiety of cyclothiazide determines the preference for flip-flop variants of AMPA receptor subunits. Neurosci.Lett. 287 161 PMID: 10854736
If you know of a relevant reference for Cyclothiazide, please let us know.
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Keywords: Cyclothiazide, Cyclothiazide supplier, AMPA, selective, desensitization, desensitisation, inhibitors, inhibits, Glutamate, Receptors, iGluR, Ionotropic, positive, allosteric, modulators, PAM, 0713, Tocris Bioscience
21 Citations for Cyclothiazide
Citations are publications that use Tocris products. Selected citations for Cyclothiazide include:
Fan et al (2018) All-optical synaptic electrophysiology probes mechanism of ketamine-induced disinhibition. Nat Methods 15 823 PMID: 30275587
McGee et al (2015) Auxiliary Subunit GSG1L Acts to Suppress Calcium-Permeable AMPA Receptor Function. Front Cell Neurosci 35 16171 PMID: 26658868
Angelantonio et al (2015) Basal adenosine modulates the functional properties of AMPA receptors in mouse hippocampal neurons through the activation of A1R A2AR and A3R. Neuropsychopharmacology 9 409 PMID: 26528137
Harms et al (2013) Functional analysis of a novel positive allosteric modulator of AMPA receptors derived from a structure-based drug design strategy. Neuropharmacology 64 45 PMID: 22735771
Kong et al (2010) Cyclothiazide induces seizure behavior in freely moving rats. Brain Res 1355 207 PMID: 20678492
Bender et al (2006) Two coincidence detectors for spike timing-dependent plasticity in somatosensory cortex. J Neurosci 26 4166 PMID: 16624937
Pieri et al (2005) AMPA receptors are modulated by tachykinins in rat cerebellum neurons. J Neurophysiol 94 2484 PMID: 16160091
Lee et al (2012) Actin-dependent rapid recruitment of reluctant synaptic vesicles into a fast-releasing vesicle pool. Proc Natl Acad Sci U S A 109 E765 PMID: 22393020
Falgairolle and O'Donovan (2015) Pharmacological Investigation of Fluoro-Gold Entry into Spinal Neurons. PLoS One 10 e0131430 PMID: 26102354
Maguire et al (2014) Extrasynaptic glycine receptors of rodent dorsal raphe serotonergic neurons: a sensitive target for ethanol. PLoS One 39 1232 PMID: 24264816
Menuz et al (2009) Critical role for TARPs in early development despite broad functional redundancy. Neuropharmacology 56 22 PMID: 18634809
Soto et al (2009) Selective regulation of long-form calcium-permeable AMPA receptors by an atypical TARP, gamma-5. Nat Neurosci 12 277 PMID: 19234459
Bretin et al (2017) Pharmacological characterisation of S 47445, a novel positive allosteric modulator of AMPA receptors. PLoS One 12 e0184429 PMID: 28886144
Seebohm et al (2014) Structural basis of PI(4,5)P2-dependent regulation of GluA1 by phosphatidylinositol-5-phosphate 4-kinase, type II, alpha (PIP5K2A). Pflugers Arch 466 1885 PMID: 24389605
Chen et al (2013) The Munc13 proteins differentially regulate readily releasable pool dynamics and calcium-dependent recovery at a central synapse. J Neurosci 33 8336 PMID: 23658173
Kopach et al (2011) Inflammation alters trafficking of extrasynaptic AMPA receptors in tonically firing lamina II neurons of the rat spinal dorsal horn. Pain 152 912 PMID: 21282008
Bagnall et al (2008) Frequency-independent synaptic transmission supports a linear vestibular behavior. Neuron 60 343 PMID: 18957225
Oh et al (2012) Overexpression of calcium-permeable glutamate receptors in glioblastoma derived brain tumor initiating cells. PLoS One 7 e47846 PMID: 23110111
Smejkalova and Woolley (2010) OE acutely potentiates hippocampal excitatory synaptic transmission through a presynaptic mechanism. J Neurosci 30 16137 PMID: 21123560
Imlach et al (2016) Glycinergic dysfunction in a subpopulation of dorsal horn interneurons in a rat model of neuropathic pain Scientific Reports 6 37104 PMID: 27841371
Takayasu et al (2006) Glial glutamate transporters maintain one-to-one relationship at the climbing fiber-Purkinje cell synapse by preventing glutamate spillover. J Neurosci 26 6563 PMID: 16775144
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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!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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.
Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.
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.