Discovery and SAR of org 24598-a selective glycine uptake inhibitor

Bioorg Med Chem Lett. 2001 Aug 6;11(15):2007-9. doi: 10.1016/s0960-894x(01)00355-9.

Abstract

The discovery of Org 24598, one of the first potent and selective inhibitors of the glycine transporter is discussed. In vitro structure-activity relationships (SARs) data for interaction of a ligand with this system is discussed.

MeSH terms

  • Amino Acid Transport Systems, Neutral*
  • Animals
  • Brain / metabolism
  • Carrier Proteins / antagonists & inhibitors*
  • Carrier Proteins / drug effects*
  • GABA Plasma Membrane Transport Proteins
  • Glycine / analogs & derivatives
  • Glycine / chemical synthesis
  • Glycine / pharmacology*
  • Glycine Plasma Membrane Transport Proteins
  • Membrane Proteins / drug effects
  • Membrane Transport Proteins*
  • Norepinephrine Plasma Membrane Transport Proteins
  • Organic Anion Transporters*
  • Radioligand Assay
  • Rats
  • Receptors, Glycine
  • Receptors, N-Methyl-D-Aspartate / agonists*
  • Sensitivity and Specificity
  • Spine / metabolism
  • Structure-Activity Relationship
  • Symporters*

Substances

  • Amino Acid Transport Systems, Neutral
  • Carrier Proteins
  • GABA Plasma Membrane Transport Proteins
  • Glycine Plasma Membrane Transport Proteins
  • Membrane Proteins
  • Membrane Transport Proteins
  • Norepinephrine Plasma Membrane Transport Proteins
  • Organic Anion Transporters
  • Receptors, Glycine
  • Receptors, N-Methyl-D-Aspartate
  • Slc6a2 protein, rat
  • Symporters
  • org 24598
  • Glycine