Chemical Name: 6-Chloro-3,4-dihydro-3-(5-norbornen-2-yl)-2H-1,2,4-benzothiazidiazine-7-sulfonamide-1,1-dioxide
Biological ActivityCyclothiazide is a positive allosteric modulator of AMPA receptors that potently inhibits AMPA receptor desensitization. Selective for the flip variant of each of the four receptor subunits.
The technical data provided above is for guidance only.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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.
Desai et al.
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.
Donevan and Rogawski
The norbornenyl moiety of cyclothiazide determines the preference for flip-flop variants of AMPA receptor subunits.
Kessler et al.
Citations for Cyclothiazide
The citations listed below are publications that use Tocris products. Selected citations for Cyclothiazide include:
21 Citations: Showing 1 - 10
All-optical synaptic electrophysiology probes mechanism of ketamine-induced disinhibition.
Authors: Fan Et al.
Nat Methods 2018;15:823
Pharmacological characterisation of S 47445, a novel positive allosteric modulator of AMPA receptors.
Authors: Bretin Et al.
PLoS One 2017;12:e0184429
Glycinergic dysfunction in a subpopulation of dorsal horn interneurons in a rat model of neuropathic pain
Authors: Imlach Et al.
Scientific Reports 2016;6:37104
Basal adenosine modulates the functional properties of AMPA receptors in mouse hippocampal neurons through the activation of A1R A2AR and A3R.
Authors: Angelantonio Et al.
Auxiliary Subunit GSG1L Acts to Suppress Calcium-Permeable AMPA Receptor Function.
Authors: McGee Et al.
Front Cell Neurosci 2015;35:16171
Pharmacological Investigation of Fluoro-Gold Entry into Spinal Neurons.
Authors: Falgairolle and O'Donovan
PLoS One 2015;10:e0131430
Structural basis of PI(4,5)P2-dependent regulation of GluA1 by phosphatidylinositol-5-phosphate 4-kinase, type II, alpha (PIP5K2A).
Authors: Seebohm Et al.
Pflugers Arch 2014;466:1885
Extrasynaptic glycine receptors of rodent dorsal raphe serotonergic neurons: a sensitive target for ethanol.
Authors: Maguire Et al.
PLoS One 2014;39:1232
Functional analysis of a novel positive allosteric modulator of AMPA receptors derived from a structure-based drug design strategy.
Authors: Harms Et al.
The Munc13 proteins differentially regulate readily releasable pool dynamics and calcium-dependent recovery at a central synapse.
Authors: Chen Et al.
J Neurosci 2013;33:8336
Overexpression of calcium-permeable glutamate receptors in glioblastoma derived brain tumor initiating cells.
Authors: Oh Et al.
PLoS One 2012;7:e47846
Actin-dependent rapid recruitment of reluctant synaptic vesicles into a fast-releasing vesicle pool.
Authors: Lee Et al.
Proc Natl Acad Sci U S A 2012;109:E765
Inflammation alters trafficking of extrasynaptic AMPA receptors in tonically firing lamina II neurons of the rat spinal dorsal horn.
Authors: Kopach Et al.
OE acutely potentiates hippocampal excitatory synaptic transmission through a presynaptic mechanism.
Authors: Smejkalova and Woolley
J Neurosci 2010;30:16137
Cyclothiazide induces seizure behavior in freely moving rats.
Authors: Kong Et al.
Brain Res 2010;1355:207
Critical role for TARPs in early development despite broad functional redundancy.
Authors: Menuz Et al.
Selective regulation of long-form calcium-permeable AMPA receptors by an atypical TARP, gamma-5.
Authors: Soto Et al.
Nat Neurosci 2009;12:277
Frequency-independent synaptic transmission supports a linear vestibular behavior.
Authors: Bagnall Et al.
Glial glutamate transporters maintain one-to-one relationship at the climbing fiber-Purkinje cell synapse by preventing glutamate spillover.
Authors: Takayasu Et al.
J Neurosci 2006;26:6563
Two coincidence detectors for spike timing-dependent plasticity in somatosensory cortex.
Authors: Bender Et al.
J Neurosci 2006;26:4166
AMPA receptors are modulated by tachykinins in rat cerebellum neurons.
Authors: Pieri Et al.
J Neurophysiol 2005;94:2484
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Cyclothiazide was used to prevent desensitization of AMPA-receptors in hippocampal pyramidal neurons. The compound prolonged the decay time of multi-synaptic evoked excitatory currents in cell somata. No difference between effects at 22-25 C and 33-36 C was detected. Illustration, grey trace: control response normalized to response amplitude under cyclothiazide.
Used to prevent desensitization AMPA receptors in motor neurons. Used at concentration of 200 micromolar to measure whole cell current in motor neurons upon AMPA application.