Variability in D2-dopamine receptor density and affinity: a PET study with [11C]raclopride in man

Synapse. 1995 Jul;20(3):200-8. doi: 10.1002/syn.890200303.

Abstract

The variability of D2-dopamine receptor binding parameters in man was determined using Positron Emission Tomography (PET) and [11C]raclopride. A saturation analysis based on five PET-experiments was performed in each of ten men and ten women. The mean density of D2-dopamine receptors (Bmax) was 28 +/- 6.9 pmol/ml (mean +/- S.D.) and the apparent affinity (Kdapp) 9.1 +/- 1.9 pmol/ml. The Hill coefficient was in all subjects close to unity (nH: 0.999 +/- 0.020), thereby indicating binding to a homogeneous class of receptors. No significant differences between males and females were found in Bmax or Kdapp. The interindividual difference in Bmax was statistically significant (alpha = 0.01). The difference in Kdapp was not significant. Upregulation of the receptor density (Bmax) has been widely discussed as a mechanism for increased dopaminergic neurotransmission in schizophrenia. This study indicates that receptor density varies considerably in a group of healthy subjects.

Publication types

  • Clinical Trial
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Adult
  • Aging / metabolism
  • Brain / anatomy & histology
  • Brain Chemistry / drug effects
  • Dopamine Antagonists* / pharmacokinetics
  • Female
  • Humans
  • Image Processing, Computer-Assisted
  • Male
  • Methylation
  • Raclopride
  • Receptors, Dopamine D2 / drug effects
  • Receptors, Dopamine D2 / metabolism*
  • Salicylamides* / pharmacokinetics
  • Sex Characteristics
  • Tomography, Emission-Computed

Substances

  • Dopamine Antagonists
  • Receptors, Dopamine D2
  • Salicylamides
  • Raclopride