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| ECHA InfoCard | 100.017.146 |
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| Formula | C14H16ClN3O4S2 |
| Molar mass | 389.87 g·mol−1 |
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Cyclothiazide (Anhydron,Acquirel,Doburil,Fluidil,Renazide,Tensodiural,Valmiran), sometimes abbreviatedCTZ, is abenzothiadiazide (thiazide)diuretic andantihypertensive that was originally introduced in the United States in 1963 byEli Lilly and was subsequently also marketed inEurope andJapan.[1][2] Relateddrugs includediazoxide,hydrochlorothiazide, andchlorothiazide.[3]
In 1993, it was discovered that cyclothiazide is apositive allosteric modulator of theAMPA andkainate receptors, capable of reducing or essentially eliminating rapiddesensitization of the former receptor, and potentiating AMPA-mediatedglutamate currents by as much as 18-fold at the highest concentration tested (100μM).[3][4][5][6] Additionally, in 2003, cyclothiazide was also found to act as aGABAA receptornegative allosteric modulator, potently inhibiting GABAA-mediated currents.[7] In animals it is a powerfulconvulsant, robustly enhancingepileptiform activity and inducingseizures, but without producing any apparentneuronal death.[8][9]
Cyclothiazide has been found to act as anon-competitive antagonist of themGluR1.[10] It is selective for mGluR1 over othermetabotropic glutamate receptors.[10]
