title: Synthesis of 3,4-dihydro-2H-1,2,4-benzo-thiadiazine 1,1-dioxide derivatives as potential allosteric modulators of AMPA/kainate receptors.
abstract: 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.
authors.forename: Daniela
authors.initials: D
authors.lastname: Braghiroli
authors.forename: Giulia
authors.initials: G
authors.lastname: Puia
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Cannazza
authors.forename: Annalisa
authors.initials: A
authors.lastname: Tait
authors.forename: Carlo
authors.initials: C
authors.lastname: Parenti
authors.forename: Gabriele
authors.initials: G
authors.lastname: Losi
authors.forename: Mario
authors.initials: M
authors.lastname: Baraldi
mesh_terms: 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
chemical_list: 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