NGB 2904 and NGB 2849: two highly selective dopamine D3 receptor antagonists

Bioorg Med Chem Lett. 1998 Oct 6;8(19):2715-8. doi: 10.1016/s0960-894x(98)00469-7.

Abstract

N-(4-[4-¿2, 3-dichlorophenyl¿-1-piperazinyl]butyl)-3-fluorenylcarboxamide and N-(4-[4-¿2, 3-dichlorophenyl¿-1-piperazinyl]butyl)-2-biphenylenylcarboxamide were prepared in several steps from 2,3-dichloroaniline. These compounds were identified as highly selective dopamine D3 receptor antagonists.

MeSH terms

  • Animals
  • CHO Cells / drug effects
  • CHO Cells / metabolism
  • Cricetinae
  • Dopamine Antagonists / chemical synthesis
  • Dopamine Antagonists / metabolism
  • Dopamine Antagonists / pharmacology*
  • Dopamine D2 Receptor Antagonists*
  • Fluorenes / chemical synthesis
  • Fluorenes / metabolism
  • Fluorenes / pharmacology*
  • Humans
  • Kinetics
  • Piperazines / chemical synthesis
  • Piperazines / metabolism
  • Piperazines / pharmacology*
  • Rats
  • Receptors, Dopamine D2 / metabolism
  • Receptors, Dopamine D3
  • Transfection

Substances

  • DRD3 protein, human
  • Dopamine Antagonists
  • Dopamine D2 Receptor Antagonists
  • Drd3 protein, rat
  • Fluorenes
  • NGB 2849
  • NGB 2904
  • Piperazines
  • Receptors, Dopamine D2
  • Receptors, Dopamine D3