PET studies on dopamine D1 receptors in the human brain with carbon-11-SCH 39166 and carbon-11-NNC 756

J Nucl Med. 1994 Dec;35(12):1916-20.

Abstract

PET studies were carried out on brain dopamine D1 receptors using two new ligands, [11C]SCH 39166 and [11C]NNC 756.

Methods: Four normal subjects and eight predominantly unilateral patients with early Parkinson's disease were investigated. Each of them underwent both a PET scan with [11C]SCH 39166 and one with [11C]NNC 756. A dose of about 185 MBq (5 mCi) of these ligands was administered intravenously and a dynamic PET scan with an ECAT 931/08 PET camera was carried out. Ratios between the striatal and cerebellar uptake of these compounds were calculated.

Results: Both [11C]SCH 39166 and [11C]NNC 756 accumulated in the striatum. There was also some neocortical binding; 75% of the striatal value in the case of [11C]SCH 39166 and 60% with [11C]NNC 756 which displayed higher (p < 0.01) uptake in the striatum than [11C]SCH 39166. There were no significant side-to-side differences in the controls nor in the parkinsonian patients.

Conclusions: These results imply that both [11C]SCH 39166 and [11C]NNC 756 can be used in PET studies for the visualization and quantification of dopamine D1 receptors. Since [11C]NNC 756 has a significantly better signal-to-noise ratio in the striatum than [11C]SCH 39166, it seems to offer definite advantages for studies of D1 receptors.

Publication types

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

MeSH terms

  • Adult
  • Aged
  • Benzazepines* / metabolism
  • Benzazepines* / pharmacokinetics
  • Benzofurans* / metabolism
  • Benzofurans* / pharmacokinetics
  • Brain / diagnostic imaging*
  • Brain / metabolism
  • Carbon Radioisotopes
  • Dopamine Antagonists*
  • Female
  • Humans
  • Kinetics
  • Male
  • Middle Aged
  • Organ Specificity
  • Parkinson Disease / diagnostic imaging*
  • Parkinson Disease / metabolism
  • Receptors, Dopamine D1 / analysis*
  • Receptors, Dopamine D1 / metabolism
  • Reference Values
  • Tomography, Emission-Computed / methods*

Substances

  • Benzazepines
  • Benzofurans
  • Carbon Radioisotopes
  • Dopamine Antagonists
  • Receptors, Dopamine D1
  • ecopipam
  • odapipam