Receptor-specific positron emission tomography radiopharmaceuticals: /sup 75/Br-labeled butyrophenone neuroleptics

Cerebral dopaminergic D/sub 2/ receptors are involved in several common disease states, such as schizophrenia, Parkinson's disease, and Huntington's chorea. The use of radiolabeled D/sub 2/ receptor-binding ligands with positron emission tomography (PET) to noninvasively quantitate D/sub 2/ receptor densities thus has potential application in medicine. Butyrophenone neuroleptics have a high in vitro and in vivo binding affinity for cerebral D/sub 2/ receptors, and due to the useful chemical and nuclear decay properties of /sup 74/Br (76% ..beta../sup +/, half-life = 1.6 h), the authors have evaluated radiobrominated bromospiperone (BSP), brombenperidol (BBP), and bromperidol (BP) as radiopharmaceuticals for use with PET.