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

E Pinard; A Alanine; A Bourson; B Büttelmann; R Gill; M Heitz; G Jaeschke; V Mutel; G Trube; R Wyler

doi:10.1016/s0960-894x(01)00392-4

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

Bioorg Med Chem Lett. 2001 Aug 20;11(16):2173-6. doi: 10.1016/s0960-894x(01)00392-4.

Authors

E Pinard¹, A Alanine, A Bourson, B Büttelmann, R Gill, M Heitz, G Jaeschke, V Mutel, G Trube, R Wyler

Affiliation

¹ Pharma Division, Discovery Chemistry, F. Hoffmann-La Roche Ltd., CH-4070, Basel, Switzerland. emmanuel.pinard@roche.com

PMID: 11514163
DOI: 10.1016/s0960-894x(01)00392-4

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.

MeSH terms

Excitatory Amino Acid Antagonists / chemical synthesis
Excitatory Amino Acid Antagonists / chemistry
Excitatory Amino Acid Antagonists / pharmacology*
Phenols / chemical synthesis
Phenols / chemistry
Phenols / pharmacology
Piperidines / chemical synthesis
Piperidines / chemistry
Piperidines / pharmacology*
Receptors, Adrenergic, alpha-1 / drug effects
Receptors, Adrenergic, alpha-1 / metabolism
Receptors, N-Methyl-D-Aspartate / antagonists & inhibitors*

Substances

1-(2-hydroxy-3-(4-hydroxy-phenyl)-propyl)-4-(4-methyl-benzyl)-piperidin-4-ol
Excitatory Amino Acid Antagonists
Phenols
Piperidines
Receptors, Adrenergic, alpha-1
Receptors, N-Methyl-D-Aspartate
Ro 25-6981