Structural analogues of some highly active non-competitive AMPA antagonists.
Some 5-methyl analogues (14a-e) of the non-competitive AMPA antagonists 3-acylated 1-(4-aminophenyl)-4-methyl-7,8-methylenedioxy-4,5-dihydro-3H-2,3-benzodi azepines (2,3) have been synthesized. Generally they show diminished or low biological activity but two derivatives (14a,b) reveal effects comparable to those of GYKI 52466 (1), the prototype non competitive AMPA antagonist.
Hámori
T
T
Institute for Drug Research, Ltd, Budapest, Hungary.
Sólyom
S
S
Berzsenyi
P
P
Andrási
F
F
Tarnawa
I
I
D000818:Animals; D014151:Anti-Anxiety Agents / Q000494:pharmacology; D000927:Anticonvulsants / Q000138:chemical synthesis / Q000494:pharmacology; D001381:Azepines / Q000138:chemical synthesis* / Q000494:pharmacology; D001522:Behavior, Animal / Q000187:drug effects; D001569:Benzodiazepines; D002545:Brain Ischemia / Q000188:drug therapy; D002478:Cells, Cultured; D002645:Chickens; D004597:Electroshock; D006801:Humans; D051379:Mice; D018408:Patch-Clamp Techniques; D011689:Purkinje Cells / Q000187:drug effects; D051381:Rats; D018091:Receptors, AMPA / Q000037:antagonists & inhibitors*; D012160:Retina / Q000187:drug effects; D013329:Structure-Activity Relationship
D014151:Anti-Anxiety Agents; D000927:Anticonvulsants; D001381:Azepines; D018091:Receptors, AMPA; C061950:GYKI 52466; D001569:Benzodiazepines