title: 2-(3,4-Dihydro-1H-isoquinolin-2yl)-pyridines as a novel class of NR1/2B subtype selective NMDA receptor antagonists.
abstract: Recently, we disclosed 4-aminoquinolines as structurally novel NR1/2B subtype selective NMDA receptor antagonists. We would now like to report our findings on structurally related pyridine analogues. The SAR developed in this series resulted in the discovery of high affinity antagonists which are selective (vs alpha1 and M1 receptors) and active in vivo.
authors.affiliation: Pharma Division, Discovery Chemistry, F. Hoffmann-La Roche Ltd., CH-4070 Basel, Switzerland. bernd.buettelmann@roche.com
authors.forename: Bernd
authors.initials: B
authors.lastname: Büttelmann
authors.forename: Alexander
authors.initials: A
authors.lastname: Alanine
authors.forename: Anne
authors.initials: A
authors.lastname: Bourson
authors.forename: Ramanjit
authors.initials: R
authors.lastname: Gill
authors.forename: Marie-Paule
authors.initials: MP
authors.lastname: Heitz
authors.forename: Vincent
authors.initials: V
authors.lastname: Mutel
authors.forename: Emmanuel
authors.initials: E
authors.lastname: Pinard
authors.forename: Gerhard
authors.initials: G
authors.lastname: Trube
authors.forename: René
authors.initials: R
authors.lastname: Wyler
mesh_terms: D000161:Acoustic Stimulation; D000818:Animals; D004305:Dose-Response Relationship, Drug; D018691:Excitatory Amino Acid Antagonists / Q000737:chemistry / Q000494:pharmacology; D006863:Hydrogen-Ion Concentration; D007546:Isoquinolines / Q000737:chemistry* / Q000494:pharmacology*; D051379:Mice; D008811:Mice, Inbred DBA; D011725:Pyridines / Q000737:chemistry* / Q000494:pharmacology*; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors*; D012640:Seizures / Q000209:etiology / Q000517:prevention & control; D013329:Structure-Activity Relationship
chemical_list: D018691:Excitatory Amino Acid Antagonists; D007546:Isoquinolines; C409466:NR1 NMDA receptor; D011725:Pyridines; D016194:Receptors, N-Methyl-D-Aspartate