Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands

Bioorg Med Chem Lett. 2001 Jun 4;11(11):1375-7. doi: 10.1016/s0960-894x(01)00241-4.

Abstract

A series of dopamine D(4) antagonists was synthesized and evaluated as potential candidates for development as positron emission tomography (PET) radioligands. All new compounds display high affinity and selectivity for the D(4) receptors and compounds 5b, 5d, and 5e were identified as candidates for radioligand development.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Binding Sites
  • Dopamine Antagonists / chemical synthesis*
  • Dopamine Antagonists / chemistry
  • Dopamine Antagonists / pharmacology
  • Dopamine D2 Receptor Antagonists*
  • Pyridines / chemical synthesis
  • Pyridines / chemistry
  • Pyridines / pharmacology
  • Pyrroles / chemical synthesis
  • Pyrroles / chemistry
  • Pyrroles / pharmacology
  • Radioligand Assay
  • Receptors, Dopamine D2 / metabolism
  • Receptors, Dopamine D4
  • Receptors, Serotonin / drug effects
  • Receptors, Serotonin / metabolism
  • Tomography, Emission-Computed / methods

Substances

  • 3-((4-(4-chlorophenyl)piperazin-1-yl)methyl)-1H-pyrrolo(2,3-b)pyridine
  • Dopamine Antagonists
  • Dopamine D2 Receptor Antagonists
  • Pyridines
  • Pyrroles
  • Receptors, Dopamine D2
  • Receptors, Serotonin
  • Receptors, Dopamine D4