[3H](+)S 14297: a novel, selective radioligand at cloned human dopamine D3 receptors

Neuropharmacology. 1995 Dec;34(12):1693-6. doi: 10.1016/0028-3908(95)00160-3.

Abstract

The selective dopamine D3 receptor antagonist [3H](+)S 14297 ((+)-[7-(N,N-dipropylamino)-5,6,7,8-tetrahydro-naphtho(2,3b)dihydro,2,3- furane]), labelled to high specific activity (145 Ci/mmol), bound to cloned human dopamine D3 receptors but displayed negligible binding to cloned human D2 receptors. [3H](+)S 14297 exhibited rapid association and dissociation, high affinity saturable binding (Kd = 7.0 nM) and a competition binding profile highly correlated with that of [125I]iodosulpride (r = 0.98).

Publication types

  • Comparative Study

MeSH terms

  • 2-Naphthylamine / analogs & derivatives*
  • 2-Naphthylamine / metabolism
  • Animals
  • Binding, Competitive
  • CHO Cells
  • Cricetinae
  • Dopamine Agents / metabolism
  • Furans / metabolism*
  • Humans
  • Ligands
  • Receptors, Dopamine D2 / metabolism*
  • Receptors, Dopamine D3
  • Sulpiride / analogs & derivatives
  • Sulpiride / metabolism
  • Transfection
  • Tritium

Substances

  • DRD3 protein, human
  • Dopamine Agents
  • Furans
  • Ligands
  • Receptors, Dopamine D2
  • Receptors, Dopamine D3
  • iodosulpride
  • Tritium
  • 7-(N,N-dipropylamino)-5,6,7,8-tetrahydronaphtho(2,3-b)dihydro-2,3-furan
  • Sulpiride
  • 2-Naphthylamine