Allosteric modulators of the AMPA receptor: novel 6-substituted dihydrophthalazines.
Novel analogs of the allosteric AMPA receptor modulator SYM 2206 have been prepared. Structure/activity correlations of these novel analogs and other dihydrophthalazines (DHPs) reveal the important contribution of the heteroatom-based aryl substituents in this class of noncompetitive inhibitors. One of the analogs (6, SYM 2189) is equipotent with the early series, but with reduced sedation.
Pei
X F
XF
Bearsden Bio, Inc., Aston, PA 19014, USA.
Sturgess
M A
MA
Valenzuela
C F
CF
Maccecchini
M L
ML
D000494:Allosteric Regulation; D000818:Animals; D002478:Cells, Cultured; D051379:Mice; D009474:Neurons / Q000187:drug effects; D010793:Phthalazines / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D018091:Receptors, AMPA / Q000187:drug effects*; D013329:Structure-Activity Relationship
D010793:Phthalazines; D018091:Receptors, AMPA