Initial experience with SPECT examinations using [123I]IBZM as a D2-dopamine receptor antagonist in Parkinson's disease

Eur J Radiol. 1991 May-Jun;12(3):182-6. doi: 10.1016/0720-048x(91)90069-8.

Abstract

[123I]IBZM is a new radioactive labelled ligand which has a high affinity and specificity to D2-dopamine receptors. The in vivo kinetics of [123I]IBZM were studied in patients with unilateral and bilateral accentuated idiopathic Parkinson's disease. The uptake in the basal ganglias and the imaging properties of this D2 receptor antagonist as a radiopharmaceutical for SPECT examinations had to be investigated. 5 patients, aged 42-66 years, (2 m/3 f) were examined. Each patient received 185 MBq [123I]IBZM intravenously. Blood samples were taken 0-120 min post injection (p.i.) and time activity curves were plotted. Three SPECT examinations were performed (I: 30-50 min; II: 50-70 min; and III: 70-90 min p.i.). The count rates (counts/pixel) in the basal ganglias and the cerebellum were measured for each SPECT series on transverse slices using the region-of-interest technique. The time-activity curve of [123I]IBZM shows a rapid decline in plasma during the first 10 min followed by a plateau until 120 min after injection. The SPECT examinations demonstrate the highest count rate in the basal ganglia during SPECT series III (i.e., 70-90 min p.i.). The side-to-side difference of the count rates were in the range of 3% in four patients, and 10% in one patient. The biokinetic data of [123I]IBZM make this substance capable as a radiopharmaceutical for SPECT examinations. The basal ganglia are best visualized 70-90 min p.i., thus [123I]IBZM seems to be a promising imaging agent for diseases of the D2-dopaminergic receptor system.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Benzamides / pharmacokinetics
  • Benzamides / pharmacology*
  • Blood-Brain Barrier
  • Brain / diagnostic imaging*
  • Brain / metabolism
  • Dopamine Antagonists*
  • Female
  • Humans
  • Male
  • Middle Aged
  • Parkinson Disease / diagnostic imaging*
  • Parkinson Disease / metabolism
  • Pyrrolidines / pharmacokinetics
  • Pyrrolidines / pharmacology*
  • Receptors, Dopamine D2
  • Tomography, Emission-Computed, Single-Photon*

Substances

  • Benzamides
  • Dopamine Antagonists
  • Pyrrolidines
  • Receptors, Dopamine D2
  • 3-iodo-2-hydroxy-6-methoxy-N-((1-ethyl-2-pyrrolidinyl)methyl)benzamide