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.

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