Cyclothiazide  (Synonyms: シクロチアジド)

Cyclothiazide is a positive allosteric modulator of ionotropic AMPA-type glutamate receptors. Cyclothiazide inhibits GABA_A receptors. Cyclothiazide is frequently used to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current. Cyclothiazide can potentiate responses to kainate in hippocampal neurons. Cyclothiazide has effects on glutamatergic neurotransmission. Cyclothiazide also induces epileptiform EEG activity accompanying behavioral seizures^[1][2][3][4].

Clyclothiazide (Compound CTZ) (0-1000 μM, 4 s) greatly potentiates AMPA currents dose-dependently and increases the peak AMPA currents by 90-fold at 100 μM (EC₅₀ = 28 μM) in GluR1-HEK cells^[1].
Clyclothiazide (100 μM, 0-150 s) inhibits the desensitization in GluR1-HEK cells much faster^[1].
Clyclothiazide (30 μM) produces marked and reversible potentiation of responses to kainate in rodent neuron patches^[2].
Clyclothiazide (100 μM) produces a leftward shift in the dose-response curve for kainate and reveals a decrease in the EC₅₀ for kainate in rodent neuron patches^[2].
Clyclothiazide (100 μM, 240 sec) completely blocks the desensitization evoked by 3 mM kainate in rodent neuron patches^[2].
Clyclothiazide (100 μM, 3 min) strongly potentiates the AMPA receptor responses as well as responses to glutamate but to a smaller extent in xenopus oocytes^[3].
Clyclothiazide (100 μM) exerts rapid desensitizing responses to glutamate through subunit-modulation in HEK293 cells^[3].
Clyclothiazide (5 μM, 48 h) results in abnormal synchronized bursting activities, with high-frequency action potentials overlaying large depolarizing shifts as well as long-term changes of the neural network properties in rodent hippocampal neurons^[4].
Clyclothiazide (20-50 μM, 1-2 h) is able to elicit epileptiform activities activities within short-term at high concentrations in rodent hippocampal neurons^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clyclothiazide (Compound CTZ) (1 M, i.c.v., single dose) results in spontaneous recurrent epileptiform bursts in urethane-anaesthetized rats^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

389.88

C₁₄H₁₆ClN₃O₄S₂

2259-96-3

Solid

White to off-white

O=S(C1=C(Cl)C=C(C2=C1)NC(C3C(C4)C=CC4C3)NS2(=O)=O)(N)=O

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Fucile S, et al. Effects of cyclothiazide on GluR1/AMPA receptors. Proc Natl Acad Sci U S A. 2006;103(8):2943-2947.  [Content Brief]

  [2]. Patneau, D. K., et al., (1993). Hippocampal neurons exhibit cyclothiazide-sensitive rapidly desensitizing responses to kainate. The Journal of neuroscience: the official journal of the Society for Neuroscience, 13(8), 3496–3509.  [Content Brief]

  [3]. Partin, K. M., et al., (1993). Selective modulation of desensitization at AMPA versus kainate receptors by cyclothiazide and concanavalin A. Neuron, 11(6), 1069–1082.  [Content Brief]

  [4]. Qi, J., et al., (2006). Cyclothiazide induces robust epileptiform activity in rat hippocampal neurons both in vitro and in vivo. The Journal of physiology, 571(Pt 3), 605–618.  [Content Brief]