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Cyclothiazide

(HB0221)
Data

Product overview

  • Name
    Cyclothiazide
  • Short description
    AMPA receptor positive allosteric modulator. Inhibits AMPAR desensitization.
  • 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.

  • Alternative names
    CTZ
  • Biological action
    PAM
  • Purity
    >98%
  • Citations

Images

Properties

  • 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]
  • 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

Applications

  • 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.

Storing and Using Your Product

  • 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.

References for Cyclothiazide

  • Effects of cyclothiazide on GluR1/AMPA receptors.

    Fucile S et al (2006) Proc Natl Acad Sci U S A 103(8) : 2943-7.
    PubMedID: 16473938
  • Downregulated GABA and BDNF-TrkB pathway in chronic cyclothiazide seizure model.

    Kong S et al (2014) Neural Plast 2014 : 310146
    PubMedID: 24757570
  • 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.
    PubMedID: 10854736
  • Superactivation of AMPA receptors by auxiliary proteins.

    Carbone and Plested (2016) Nat Commun 7 : 10178. doi: 10.1038/ncomms1017
    PubMedID: 26744192
Our products in action
The following papers have cited the use of Cyclothiazide (HB0221) from Hello Bio. If you have published a paper using this product, and it is not shown here, then please tell us! We will send you a free gift as a thank you!
  • Superactivation of AMPA receptors by auxiliary proteins.

    Carbone and Plested(2016) Nat Commun 7 : 10178. doi: 10.1038/ncomms1017
    PubMedID: 26744192
  • Unitary Properties of AMPA Receptors with Reduced Desensitization

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