[76Br]bromolisuride: a new tool for quantitative in vivo imaging of D-2 dopamine receptors

Eur J Pharmacol. 1986 Aug 15;127(3):239-47. doi: 10.1016/0014-2999(86)90370-5.

Abstract

Bromolisuride, an ergoline derivative, was labeled with the positron emitter radionuclide, bromine 76. In vitro and in vivo binding and competition studies in rats demonstrated a high affinity (KD = 0.3 nM) and a high specificity of this new radioligand for D-2 dopamine receptors. PET kinetic studies in baboons showed an accumulation of [76Br]bromolisuride in the striatum which reached a maximum 30 min post-injection and which could be displaced by haloperidol. All these results indicated that this new ligand is certainly suitable for the non-invasive in vivo quantitative imaging of D-2 dopamine receptor sites in human brain.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Brain / metabolism*
  • Bromine
  • Corpus Striatum / metabolism
  • Ergolines / metabolism*
  • Lisuride / analogs & derivatives
  • Lisuride / metabolism*
  • Male
  • Papio
  • Radioisotopes
  • Rats
  • Rats, Inbred Strains
  • Receptors, Dopamine / metabolism*
  • Receptors, Dopamine D2
  • Tomography, Emission-Computed

Substances

  • Ergolines
  • Radioisotopes
  • Receptors, Dopamine
  • Receptors, Dopamine D2
  • Lisuride
  • bromerguride
  • Bromine