A novel class of allosteric modulators of AMPA/Kainate receptors.
The rapid hydrolysis in vivo of IDRA21 to 2-amino-5-chlorobenzensulfonamide has been demonstrated by microdialysis experiments. The IDRA21 metabolite possess in vitro a biological activity similar to that of IDRA21 itself. Taking 2-amino-5-chlorobenzensulfonamide as lead compound, a novel class of AMPAR positive allosteric modulators has been prepared.
Cannazza
Giuseppe
G
Department of Pharmaceutical Science, University of Modena e Reggio Emilia, Via Campi 183, 41100 Modena, Italy. giuseppe.cannazza@unimo.it
Jozwiak
Krzysztof
K
Parenti
Carlo
C
Braghiroli
Daniela
D
Carrozzo
Marina M
MM
Puia
Giulia
G
Losi
Gabriele
G
Baraldi
Mario
M
Lindner
Wolfgang
W
Wainer
Irving W
IW
D000284:Administration, Oral; D000818:Animals; D001581:Benzothiadiazines / Q000737:chemistry / Q000494:pharmacology*; D020650:Combinatorial Chemistry Techniques; D006624:Hippocampus / Q000187:drug effects; D008958:Models, Molecular; D015394:Molecular Structure; D051381:Rats; D018091:Receptors, AMPA / Q000187:drug effects*; D018092:Kainic Acid Receptors / Q000187:drug effects*; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000096926:Benzenesulfonamides
D001581:Benzothiadiazines; D018091:Receptors, AMPA; D018092:Kainic Acid Receptors; D013449:Sulfonamides; D000096926:Benzenesulfonamides; C538710:2-amino-5-chlobenzensulfonamide; C091420:IDRA 21