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 compa...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2000-05, Vol.10 (9), p.899-902
Hauptverfasser:	Hámori, T, Sólyom, S, Berzsenyi, P, Andrási, F, Tarnawa, I
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Anti-Anxiety Agents - pharmacology Anticonvulsants - chemical synthesis Anticonvulsants - pharmacology Azepines - chemical synthesis Azepines - pharmacology Behavior, Animal - drug effects Benzodiazepines Brain Ischemia - drug therapy Cells, Cultured Chickens Electroshock Humans Mice Patch-Clamp Techniques Purkinje Cells - drug effects Rats Receptors, AMPA - antagonists & inhibitors Retina - drug effects Structure-Activity Relationship
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Zusammenfassung:	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.
ISSN:	0960-894X
DOI:	10.1016/S0960-894X(00)00117-7