title: Benzobistriazinones and related heterocyclic ring systems as potent, orally bioavailable positive allosteric AMPA receptor modulators.
abstract: AMPA receptors (AMPARs) are an important therapeutic target in the CNS. A series of substituted benzobistriazinone, benzobispyrimidinone and related derivatives have been prepared with high potency and selectivity for the allosteric binding site of AMPARs. Further improvements have been made to previously reported series of positive AMPAR modulators and these compounds exhibit excellent in vivo activity and improved in vivo metabolic stability with up to 100% oral bioavailability in rat.
authors: Cortex Pharmaceuticals Inc., 15231 Barranca Parkway, Irvine, CA 92618, USA. rudolfmueller@yahoo.com
authors: Rudolf
authors: R
authors: Mueller
authors: Stanislaw
authors: S
authors: Rachwal
authors: Mark A
authors: MA
authors: Varney
authors: Steven A
authors: SA
authors: Johnson
authors: Kashinatham
authors: K
authors: Alisala
authors: Sheng
authors: S
authors: Zhong
authors: Yong-Xin
authors: YX
authors: Li
authors: Peter
authors: P
authors: Haroldsen
authors: Todd
authors: T
authors: Herbst
authors: Leslie J
authors: LJ
authors: Street
mesh_terms: D000284:Administration, Oral; D000494:Allosteric Regulation; D000818:Animals; D001665:Binding Sites; D006571:Heterocyclic Compounds / Q000737:chemistry*; D051381:Rats; D018091:Receptors, AMPA / Q000737:chemistry* / Q000378:metabolism; D014227:Triazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics
chemical_list: D006571:Heterocyclic Compounds; D018091:Receptors, AMPA; D014227:Triazines