[76Br]bromolisuride: a new tool for quantitative in vivo imaging of D-2 dopamine receptors.
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.
D000818:Animals; D001921:Brain / Q000378:metabolism*; D001966:Bromine; D003342:Corpus Striatum / Q000378:metabolism; D004873:Ergolines / Q000378:metabolism*; D008090:Lisuride / Q000031:analogs & derivatives / Q000378:metabolism*; D008297:Male; D010215:Papio; D011868:Radioisotopes; D051381:Rats; D011919:Rats, Inbred Strains; D011954:Receptors, Dopamine / Q000378:metabolism*; D017448:Receptors, Dopamine D2; D014055:Tomography, Emission-Computed
D004873:Ergolines; D011868:Radioisotopes; D011954:Receptors, Dopamine; D017448:Receptors, Dopamine D2; D008090:Lisuride; C039667:bromerguride; D001966:Bromine