title: Discovery of (R)-1-[2-hydroxy-3-(4-hydroxy-phenyl)-propyl]-4-(4-methyl-benzyl)-piperidin-4-ol: a novel NR1/2B subtype selective NMDA receptor antagonist.
abstract: Starting from Ro-25-6981 as a lead compound, highly potent and selective NR1/2B subtype selective NMDA receptor antagonists, with low activity at alpha(1) adrenergic receptors were developed.
authors.affiliation: Pharma Division, Discovery Chemistry, F. Hoffmann-La Roche Ltd., CH-4070, Basel, Switzerland. emmanuel.pinard@roche.com
authors.forename: E
authors.initials: E
authors.lastname: Pinard
authors.forename: A
authors.initials: A
authors.lastname: Alanine
authors.forename: A
authors.initials: A
authors.lastname: Bourson
authors.forename: B
authors.initials: B
authors.lastname: Büttelmann
authors.forename: R
authors.initials: R
authors.lastname: Gill
authors.forename: M
authors.initials: M
authors.lastname: Heitz
authors.forename: G
authors.initials: G
authors.lastname: Jaeschke
authors.forename: V
authors.initials: V
authors.lastname: Mutel
authors.forename: G
authors.initials: G
authors.lastname: Trube
authors.forename: R
authors.initials: R
authors.lastname: Wyler
mesh_terms: D018691:Excitatory Amino Acid Antagonists / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D010636:Phenols / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D010880:Piperidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D018340:Receptors, Adrenergic, alpha-1 / Q000187:drug effects / Q000378:metabolism; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors*
chemical_list: C435645:1-(2-hydroxy-3-(4-hydroxy-phenyl)-propyl)-4-(4-methyl-benzyl)-piperidin-4-ol; D018691:Excitatory Amino Acid Antagonists; D010636:Phenols; D010880:Piperidines; D018340:Receptors, Adrenergic, alpha-1; D016194:Receptors, N-Methyl-D-Aspartate; C109643:Ro 25-6981