Analogues of the dopamine D2 receptor antagonist L741,626: Binding, function, and SAR

Bioorg Med Chem Lett. 2007 Feb 1;17(3):745-9. doi: 10.1016/j.bmcl.2006.10.076. Epub 2006 Oct 28.

Abstract

A series of analogues of the dopamine D2 receptor antagonist L741,626 were synthesized and evaluated for binding and function at D2 family receptor subtypes. Several analogues showed comparable binding profiles to the parent ligand, however, in general, chemical modification served to reduce D2 binding affinity and selectivity.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, N.I.H., Intramural

MeSH terms

  • Cell Line
  • Dopamine Antagonists / chemical synthesis*
  • Dopamine Antagonists / pharmacology*
  • Humans
  • Indoles / chemical synthesis*
  • Indoles / pharmacology*
  • Ligands
  • Piperidines / chemical synthesis*
  • Piperidines / pharmacology*
  • Protein Binding
  • Receptors, Dopamine D2 / drug effects*
  • Receptors, Dopamine D2 / genetics
  • Structure-Activity Relationship
  • Transfection

Substances

  • Dopamine Antagonists
  • Indoles
  • Ligands
  • Piperidines
  • Receptors, Dopamine D2
  • 3-(4-(4-chlorophenyl-4-hydroxypiperidino)methyl)indole