Cyclothiazide

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