Relative affinities of dopaminergic drugs at dopamine D2 and D3 receptors

Eur J Pharmacol. 1995 May 24;278(3):243-7. doi: 10.1016/0014-2999(95)00160-m.

Abstract

Quantitative autoradiography was used to evaluate the pharmacological profile of dopamine D2-like receptors labeled by [125I]iodosulpiride. Caudate/putamen, a brain region associated primarily with dopamine D2 receptor mRNA, was used as a prototypical D2 tissue; cerebellar lobule X (D3 mRNA associated), as a D3 tissue. 7-OH-DPAT ((+/-)-2-dipropylamino-7-hydroxy-1,2,3,4- tetrahydronaphthalene) exhibited selectively for cerebellar receptors (24-fold), followed by quinpirole (6-fold). Haloperidol and domperidone were 4- and 18-fold more potent at striatal receptors, respectively. These data are in close agreement with that derived from dopamine D2 and D3 receptor-expressing cell lines.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Autoradiography
  • Binding, Competitive
  • Brain / ultrastructure*
  • CHO Cells / ultrastructure
  • Caudate Nucleus / ultrastructure
  • Cerebellum / ultrastructure
  • Cricetinae
  • Dopamine Agents / metabolism*
  • Iodine Radioisotopes
  • Male
  • Putamen / ultrastructure
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Dopamine / metabolism*
  • Receptors, Dopamine D2 / metabolism*
  • Receptors, Dopamine D3
  • Sensitivity and Specificity
  • Sulpiride / analogs & derivatives
  • Sulpiride / metabolism
  • Tetrahydronaphthalenes / metabolism

Substances

  • Dopamine Agents
  • Drd3 protein, rat
  • Iodine Radioisotopes
  • Receptors, Dopamine
  • Receptors, Dopamine D2
  • Receptors, Dopamine D3
  • Tetrahydronaphthalenes
  • iodosulpride
  • Sulpiride
  • 7-hydroxy-2-N,N-dipropylaminotetralin