title: 1-Benzyloxy-4,5-dihydro-1H-imidazol-2-yl-amines, a novel class of NR1/2B subtype selective NMDA receptor antagonists.
abstract: Screening of the Roche compound depository led to the identification of (1-benzyloxy-4,5-dihydro-1H-imidazol-2-yl)-butyl amine 4, a structurally novel NR1/2B subtype selective NMDA receptor antagonist. The structure-activity relationships developed in this series resulted in the discovery of a novel class of potent and selective NMDA receptor blockers displaying activity in vivo.
authors.affiliation: Pharma Division, Discovery Chemistry, F. Hoffmann-La Roche Ltd., CH-4070 Basel, Switzerland. alexander.alanine@roche.com
authors.forename: Alexander
authors.initials: A
authors.lastname: Alanine
authors.forename: Anne
authors.initials: A
authors.lastname: Bourson
authors.forename: Bernd
authors.initials: B
authors.lastname: Büttelmann
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: D000818:Animals; D002478:Cells, Cultured; D018691:Excitatory Amino Acid Antagonists / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology; D007093:Imidazoles / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology; D007274:Injections, Intraperitoneal; D051379:Mice; D008811:Mice, Inbred DBA; D024642:Potassium Channels, Voltage-Gated / Q000037:antagonists & inhibitors; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors* / Q000502:physiology; D012640:Seizures / Q000517:prevention & control
chemical_list: D018691:Excitatory Amino Acid Antagonists; D007093:Imidazoles; C409466:NR1 NMDA receptor; C121001:NR2B NMDA receptor; D024642:Potassium Channels, Voltage-Gated; D016194:Receptors, N-Methyl-D-Aspartate