Determination of dopamine D(4) receptor density in rat striatum using PB12 as a probe

Eur J Pharmacol. 2001 Sep 7;427(1):1-5. doi: 10.1016/s0014-2999(01)01129-3.

Abstract

N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide (PB12), a potent and selective dopamine D(4) receptor ligand, was used as a probe for the direct determination of the dopamine D(4) receptor density in rat striatum as an alternative to the subtraction method. The experiment was performed using [(3)H]spiroperidol to label D(2), D(3) and D(4) receptors and PB12 to determine directly dopamine D(4) receptor specific binding. The determined B(max) value was 82 fmol/mg protein. The contribution of the dopamine D(4) receptor to the overall population of D(2)-like receptors was 63%; however, this value cannot be considered reliable because of the observed difference in the kinetic profiles of D(2), D(3) and D(4) receptors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Benzamides / metabolism*
  • Benzamides / pharmacology
  • Binding, Competitive / drug effects
  • Corpus Striatum / drug effects
  • Corpus Striatum / metabolism*
  • Dose-Response Relationship, Drug
  • Haloperidol / pharmacology
  • Kinetics
  • Male
  • Membranes / drug effects
  • Membranes / metabolism
  • Piperazines / metabolism*
  • Piperazines / pharmacology
  • Radioligand Assay
  • Rats
  • Rats, Wistar
  • Receptors, Dopamine D2 / metabolism*
  • Receptors, Dopamine D4
  • Spiperone / metabolism
  • Time Factors
  • Tritium

Substances

  • Benzamides
  • Drd4 protein, rat
  • N-(2-(4-(4-chlorophenyl)piperazin-1-yl)ethyl)-3-methoxybenzamide
  • Piperazines
  • Receptors, Dopamine D2
  • Tritium
  • Receptors, Dopamine D4
  • Spiperone
  • Haloperidol