Sm. Moerlein et al., SPECIFIC, REVERSIBLE BINDING OF [F-18] BENPERIDOL TO BABOON D-2 RECEPTORS - PET EVALUATION OF AN IMPROVED F-18 LABELED LIGAND, Nuclear medicine and biology, 22(6), 1995, pp. 809-815
[F-18]Benperidol ([F-18]BP), a positron-emitting analogue of the dopam
inergic D-2 antagonist benperidol, was evaluated as a radiopharmaceuti
cal for use with positron emission tomography (PET). PET imaging of ba
boons after i.v. injection of [F-18]BP indicated that the radiofluorin
ated ligand rapidly localized in vivo within dopaminergic receptor-ric
h cerebral tissues, and that selective disposition was retained for ov
er 2 h. Pretreatment of an animal with unlabeled receptor-specific ant
agonists prior to injection of [F-18]BP confirmed that the radioligand
bound specifically to central D-2 receptors in vivo, and not to S-2 o
r D-1 receptors. [F-18]BP bound to D-2 receptors in a reversible manne
r; unlabeled eticlopride displaced D-2 receptor-bound [F-18]BP in vivo
. The radioligand was metabolized in the periphery to polar metabolite
s which are not expected to cross the blood-brain barrier. [F-18]BP ha
s advantages over other tracers as a radiopharmaceutical for PET study
of central D-2 receptor activity, and can be applied for noninvasive
evaluation of the interaction of unlabeled drugs with central D-2 rece
ptor sites.