Preparation of 11C-labelled Raclopride, a new potent dopamine receptor antagonist: preliminary PET studies of cerebral dopamine receptors in the monkey

Int J Appl Radiat Isot. 1985 Apr;36(4):269-73. doi: 10.1016/0020-708x(85)90083-3.

Abstract

A new dopamine receptor antagonist, Raclopride (S-(-)-3,5-dichloro-N-[(1-ethyl-2-pyrrolidinyl)]methyl-2-hydroxy- 6-methoxybenzamide, FLA 870) (1), has been labelled using [11C]ethyl iodide for alkylation of the nitrogen of the pyrrolidine ring in the corresponding secondary amine (5). The synthesis of 5 and an efficient method for the preparation of [11C]ethyl iodide are described. The 11C-labelled FLA 870 (1) was purified by HPLC and then used in positron emission tomography to visualize the dopamine receptor-rich areas of the monkey brain. The images obtained show selective accumulation of FLA 870 in striatum and a 10-fold separation between the binding to caudate vs cerebellum.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Benzamides*
  • Brain / diagnostic imaging*
  • Carbon Radioisotopes*
  • Isotope Labeling / methods
  • Macaca fascicularis
  • Raclopride
  • Receptors, Dopamine / analysis*
  • Tomography, Emission-Computed*

Substances

  • Benzamides
  • Carbon Radioisotopes
  • Receptors, Dopamine
  • Raclopride