Product overview

• NameCyclothiazide
• Short descriptionAMPA receptor positive allosteric modulator. Inhibits AMPAR desensitization.
• Biological descriptionAMPA receptor positive allosteric modulator (PAM). Produces a fast inhibition of AMPAR desensitization and a slow potentiation of the AMPA current. Also inhibits GABA_A mediated currents. Shows diuretic and convulsive actions. Active in vivo.
• Alternative namesCTZ
• Biological actionPAM
• Purity>98%
• Our products in action2 citationsSubmit Your Citation Now

Images

Properties

• Chemical name6-Chloro-3,4-dihydro-3-(5-norbornen-2-yl)-2H-1,2,4-benzothiazidiazine-7-sulfonamide-1 ,1-dioxide
• Molecular Weight389.87
• Chemical structure
• Molecular FormulaC₁₄H₁₆ClN₃O₄S₂
• CAS Number2259-96-3
• PubChem identifier2910
• SMILESC1C2CC(C1C=C2)C3NC4=CC(=C(C=C4S(=O)(=O)N3)S(=O)(=O)N)Cl
• SourceSynthetic
• InChiInChI=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)
• InChiKeyBOCUKUHCLICSIY-UHFFFAOYSA-N
• MDL numberMFCD00210192
• AppearanceWhite 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 instructionsRoom temperature
• Solubility overviewSoluble in DMSO (100mM) or ethanol (25mM)
• ImportantThis 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