Cyclothiazide

Cyclothiazide (CAS No.: 2259-96-3) is a thiazide compound that was initially introduced into clinical use as a diuretic and antihypertensive drug. Subsequent studies have found that it has significant neuromodulatory effects, particularly as a positive allosteric modulator of AMPA receptors, effectively inhibiting AMPA receptor desensitization and enhancing current responses. AMPA receptors are composed of the GluR-1, GluR-2, GluR-3, and GluR-4 subunits, and Cyclothiazide is selective for the flip variants of these subunits. In vitro studies show that Cyclothiazide can significantly enhance AMPA receptor-mediated synaptic transmission at nanomolar to low micromolar concentrations. The dose or concentration used in experiments typically depends on the experimental design and research objectives. In cellular and animal models, Cyclothiazide is commonly used to study AMPA receptor function, synaptic plasticity, and mechanisms related to neurodegenerative diseases. In addition, in drug screening studies, Cyclothiazide is used as a reference compound to evaluate the potency and selectivity of other AMPA receptor modulators.