Synthesis of 3,4-dihydro-2H-1,2,4-benzo-thiadiazine 1,1-dioxide derivatives as potential allosteric modulators of AMPA/kainate receptors.
A series of 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide derivatives were synthesized and evaluated for their activity as allosteric modulators of kainate-activated currents in primary cultures of cerebellar granule neurons. Substitution of different groups at the 3-position of the benzothiadiazine ring distinguished between positive and negative allosteric modulatory properties.
Braghiroli
Daniela
D
Puia
Giulia
G
Cannazza
Giuseppe
G
Tait
Annalisa
A
Parenti
Carlo
C
Losi
Gabriele
G
Baraldi
Mario
M
D000494:Allosteric Regulation; D000818:Animals; D001581:Benzothiadiazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002460:Cell Line; D002531:Cerebellum / Q000166:cytology; D018690:Excitatory Amino Acid Agonists / Q000494:pharmacology; D007608:Kainic Acid / Q000494:pharmacology; D018408:Patch-Clamp Techniques; D051381:Rats; D018091:Receptors, AMPA / Q000187:drug effects* / Q000502:physiology; D018092:Kainic Acid Receptors / Q000187:drug effects* / Q000502:physiology; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D001581:Benzothiadiazines; D018690:Excitatory Amino Acid Agonists; D007608:Kainic Acid; D018091:Receptors, AMPA; D018092:Kainic Acid Receptors; C425327:3,4-dihydro-1,2,4-benzothiadiazine-1,1-dioxide