Iodoethylspiperone, a new potential agent for exploration of central dopamine D2 receptors: synthesis and preliminary in vivo study

Int J Rad Appl Instrum B. 1990;17(4):389-95. doi: 10.1016/0883-2897(90)90106-b.

Abstract

We synthesized a new spiperone derivative: iodoethylspiperone (IES) to perform dopamine D2 receptor exploration by SPECT. IES was prepared from a precursor: tosylethylspiperone, and characterized by i.r. and 1H-NMR analyses. [125I]IES was obtained with 80% yield. In vivo biodistribution in rats showed a high and specific uptake in the striatum. The uptake ratio between the striatum and the cerebellum reached a maximum value 4 h after injection (10.05 +/- 2.81). IES labeled with 123I should be a promising new agent to investigate D2 receptors in the living human brain.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Brain / diagnostic imaging
  • Brain / metabolism*
  • Cerebellum / diagnostic imaging
  • Cerebellum / metabolism
  • Corpus Striatum / diagnostic imaging
  • Corpus Striatum / metabolism
  • Iodine Radioisotopes
  • Male
  • Rats
  • Rats, Inbred Strains
  • Receptors, Dopamine D2
  • Receptors, Dopamine*
  • Spiperone / analogs & derivatives*
  • Spiperone / chemical synthesis
  • Spiperone / pharmacokinetics
  • Tomography, Emission-Computed

Substances

  • Iodine Radioisotopes
  • Receptors, Dopamine
  • Receptors, Dopamine D2
  • iodoethylspiperone
  • Spiperone