1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. iGluR GABA Receptor
  3. Cyclothiazide

Cyclothiazide is a positive allosteric modulator of ionotropic AMPA-type glutamate receptors. Cyclothiazide inhibits GABAA 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.

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Cyclothiazide Chemical Structure

Cyclothiazide Chemical Structure

CAS No. : 2259-96-3

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Description

Cyclothiazide is a positive allosteric modulator of ionotropic AMPA-type glutamate receptors. Cyclothiazide inhibits GABAA 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].

IC50 & Target

AMPA Receptor

 

Cellular Effect
Cell Line Type Value Description References
HEK293 EC50
> 100 μM
Compound: CTZ, Cyclothiazide
Activity at human recombinant GluA2 receptor flop isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
Activity at human recombinant GluA2 receptor flop isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
[PMID: 20096591]
HEK293 EC50
13.7 μM
Compound: CTZ, Cyclothiazide
Activity at human recombinant GluA3 receptor flip isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
Activity at human recombinant GluA3 receptor flip isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
[PMID: 20096591]
HEK293 EC50
19.8 μM
Compound: CTZ, Cyclothiazide
Activity at human recombinant GluA1 receptor flip isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
Activity at human recombinant GluA1 receptor flip isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
[PMID: 20096591]
HEK293 EC50
2.24 μM
Compound: CTZ, Cyclothiazide
Activity at human recombinant GluA2 receptor flip isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
Activity at human recombinant GluA2 receptor flip isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
[PMID: 20096591]
HEK293 EC50
3.91 μM
Compound: CTZ, Cyclothiazide
Activity at human recombinant GluA4 receptor flip isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
Activity at human recombinant GluA4 receptor flip isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
[PMID: 20096591]
HEK293 EC50
3800 nM
Compound: 2, cyclothiazide
Activity against human GLUR4 flip expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay
Activity against human GLUR4 flip expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay
[PMID: 16879964]
HEK293 EC50
7.6 μM
Compound: cyclothiazide
Agonist activity at human GluA2(Q)i expressed in HEK293 cells assessed as enhancement of glutamate-evoked desensitized current by whole cell patch clamp method
Agonist activity at human GluA2(Q)i expressed in HEK293 cells assessed as enhancement of glutamate-evoked desensitized current by whole cell patch clamp method
[PMID: 26653877]
Oocyte EC50
10 μM
Compound: CTZ, Cyclothiazide
Activity at recombinant GluA1 receptor flop isoform expressed in Xenopus oocytes co-expressing gamma2-TARP assessed as effect on 10 uM glutamate-induced current by voltage-clamp electrophysiological assay
Activity at recombinant GluA1 receptor flop isoform expressed in Xenopus oocytes co-expressing gamma2-TARP assessed as effect on 10 uM glutamate-induced current by voltage-clamp electrophysiological assay
[PMID: 20096591]
Oocyte EC50
2 μM
Compound: CTZ, Cyclothiazide
Activity at recombinant GluA1 receptor flip isoform expressed in Xenopus oocytes co-expressing gamma2-TARP assessed as effect on 10 uM glutamate-induced current by voltage-clamp electrophysiological assay
Activity at recombinant GluA1 receptor flip isoform expressed in Xenopus oocytes co-expressing gamma2-TARP assessed as effect on 10 uM glutamate-induced current by voltage-clamp electrophysiological assay
[PMID: 20096591]
Oocyte EC50
7.6 μM
Compound: Cyclothiazide
Agonist activity at rat flip iGluR2(Q) expressed in Xenopus laevis oocytes by whole cell patch-clamp method
Agonist activity at rat flip iGluR2(Q) expressed in Xenopus laevis oocytes by whole cell patch-clamp method
[PMID: 18811139]
In Vitro

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.

In Vivo

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.

Molecular Weight

389.88

Formula

C14H16ClN3O4S2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (320.61 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5649 mL 12.8245 mL 25.6489 mL
5 mM 0.5130 mL 2.5649 mL 5.1298 mL
View the Complete Stock Solution Preparation Table

* 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.

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Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.29%

References

Complete Stock Solution Preparation Table

* 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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5649 mL 12.8245 mL 25.6489 mL 64.1223 mL
5 mM 0.5130 mL 2.5649 mL 5.1298 mL 12.8245 mL
10 mM 0.2565 mL 1.2824 mL 2.5649 mL 6.4122 mL
15 mM 0.1710 mL 0.8550 mL 1.7099 mL 4.2748 mL
20 mM 0.1282 mL 0.6412 mL 1.2824 mL 3.2061 mL
25 mM 0.1026 mL 0.5130 mL 1.0260 mL 2.5649 mL
30 mM 0.0855 mL 0.4275 mL 0.8550 mL 2.1374 mL
40 mM 0.0641 mL 0.3206 mL 0.6412 mL 1.6031 mL
50 mM 0.0513 mL 0.2565 mL 0.5130 mL 1.2824 mL
60 mM 0.0427 mL 0.2137 mL 0.4275 mL 1.0687 mL
80 mM 0.0321 mL 0.1603 mL 0.3206 mL 0.8015 mL
100 mM 0.0256 mL 0.1282 mL 0.2565 mL 0.6412 mL
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Product Name:
Cyclothiazide
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