Cyclothiazide

(HB0221)
Technical documents: SDS CoA Datasheet

Product overview

Name Cyclothiazide
Description AMPA receptor positive allosteric modulator. Inhibits AMPAR desensitization.
Alternative names CTZ
Purity >98%
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Cyclothiazide inhibition of AMPA receptor mediated EPSCs
Cyclothiazide: Scientist Approved
Cyclothiazide - vial

Biological Data

Biological description

Cyclothiazide (CTZ) is an AMPA receptor positive allosteric modulator (PAM) which produces a fast inhibition of AMPAR desensitization and a slow potentiation of the AMPA current.

Cyclothiazide also inhibits GABAA mediated currents and shows diuretic and convulsive actions.

Cyclothiazide is active in vivo.

Application notes

The AMPAR positive allosteric modulator Cyclothiazide increases the open time of the AMPAR by inhibiting AMPAR desensitization. It is often used at a concentration of 100 μM. Cyclothiazide from Hello Bio potentiates AMPAR mediated evoked EPSCs in cortical neurons at 50 μM and above (see Fig 1 above)

 

#Protocol 1: Evoked and spontaneous evoked excitatory post synaptic currents (EPSCs)

  • Whole cell voltage clamp recordings were obtained from layer V neurons of the mouse prelimbic cortex brain slice.
  • EPSCs were evoked via a stimulating electrode placed in layers II/III delivering a single square (150 μs) pulse every 10 sec at an intensity that gave a reliable EPSC. 
  • Neurons were held at -70 mV (the reversal potential of GABA currents).
  • EPSCs were then continuously stimulated and recorded in response to 5 min applications of 50 μM and then 100 μM Cyclothiazide.

Solubility & Handling

Storage instructions Room temperature
Solubility overview Soluble in DMSO (100mM) or ethanol (25mM)
Important This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.

Calculators

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Dilution

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Chemical Data

Chemical name 6-Chloro-3,4-dihydro-3-(5-norbornen-2-yl)-2H-1,2,4-benzothiazidiazine-7-sulfonamide-1 ,1-dioxide
Molecular Weight 389.87
Chemical structure Cyclothiazide  [2259-96-3] Chemical Structure
Molecular Formula C14H16ClN3O4S2
CAS Number 2259-96-3
PubChem identifier 2910
SMILES C1C2CC(C1C=C2)C3NC4=CC(=C(C=C4S(=O)(=O)N3)S(=O)(=O)N)Cl
Source Synthetic
InChi InChI=1S/C14H16ClN3O4S2/c15-10-5-11-13(6-12(10)23(16,19)20)24(21,22)18-14(17-11)9-4-7-1-2-8(9)3-7/h1-2,5-9,14,17-18H,3-4H2,(H2,16,19,20)
InChiKey BOCUKUHCLICSIY-UHFFFAOYSA-N
MDL number MFCD00210192
Appearance White solid

References for Cyclothiazide

References are publications that support the biological activity of the product
  • Superactivation of AMPA receptors by auxiliary proteins.

    Carbone and Plested (2016) Nat Commun 7 : 10178. doi: 10.1038/ncomms1017
  • Downregulated GABA and BDNF-TrkB pathway in chronic cyclothiazide seizure model.

    Kong S et al (2014) Neural Plast 2014 : 310146
  • Effects of cyclothiazide on GluR1/AMPA receptors.

    Fucile S et al (2006) Proc Natl Acad Sci U S A 103(8) : 2943-7.
  • The norbornenyl moiety of cyclothiazide determines the preference for flip-flop variants of AMPA receptor subunits.

    Kessler M et al (2000) Neurosci Lett 287(2) : 161-5.
Publications
These publications cite the use of Cyclothiazide purchased from Hello Bio:
  • Mutational Analysis and Modeling of Negative Allosteric Modulator Binding Sites in AMPA Receptors

    Stenum-Berg et al (2019) Mol Pharmacol. 835-850 : 96(6)
    PubMedID: 31582576
  • Auxiliary subunits keep AMPA receptors compact during activation and desensitization

    Baranovic and Plested (2018) bioRxiv https://doi.org : /10.1101/295105
  • Calcium rises induced by AMPA and nicotine receptors in the ventral tegmental area show differences in mouse brain slices prenatally exposed to nicotine.

    Ipsen et al (2018) Dev Neurobiol doi:10. : 1002/dneu.22607.
    PubMedID: 29923678
  • Degeneration of cholinergic basal forebrain nuclei after focally evoked status epilepticus.

    Biagioni et al (2018) Neurobiol Dis. pii: S0969-9961(18)30609-0. : doi: 10.1016/j.nbd.2018.09.019.
    PubMedID: 30243733
  • Unitary Properties of AMPA Receptors with Reduced Desensitization

    Zhang W et al (2017) Biophys J S0006-3495 : 30856-1
    PubMedID: 28863863

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