Comparison of D2 and D3 dopamine receptor affinity of dopaminergic compounds in rat brain

Life Sci. 1998;62(20):1825-31. doi: 10.1016/s0024-3205(98)00148-9.

Abstract

This study used quantitative autoradiography to simultaneously evaluate the relative affinities of dopaminergic compounds for dopamine D2 and D3 receptors in rat brain. PD 152255, PD 128907, and l-nafadotride exhibited significantly higher affinity for cerebellar dopamine D3 sites than [3H]quinpirole-labeled sites in caudate/putamen (6.3-, 6.0-, and 2.3-fold, respectively). In contrast, chlorpromazine, risperidone, and domperidone were more potent at striatal dopamine D2 receptors (3.8-, 31-, and 40-fold, respectively). Dopamine, quinelorane, (+)-UH 232, and RS-trans-7-OH-PIPAT exhibited relatively little D2/D3 selectivity.

Publication types

  • Comparative Study
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Autoradiography
  • Binding, Competitive
  • Brain / drug effects
  • Brain / metabolism*
  • Dopamine Agonists / metabolism*
  • Dopamine Agonists / pharmacology
  • Dopamine Antagonists / metabolism*
  • Dopamine Antagonists / pharmacology
  • Male
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Dopamine D2 / metabolism*
  • Receptors, Dopamine D3

Substances

  • Dopamine Agonists
  • Dopamine Antagonists
  • Drd3 protein, rat
  • Receptors, Dopamine D2
  • Receptors, Dopamine D3