TY - JOUR
T1 - Specific binding of 3N-(2′-[18F]fluoroethyl)benperidol to primate cerebral dopaminergic D2 receptors demonstrated in vivo by PET
AU - Moerlein, Stephen M.
AU - Perlmutter, Joel S.
N1 - Funding Information:
We are grateful to L. Lich and J. Carl for exert technical assistance with the animal studies, J. Hood for data processing, W. Margenau and J. Robison for radioisotope production, and L. Carver for manuscript preparation. This work was supported by the McDonnell Center for the Study of Higher Brain Function, NIH FIRST Award 1R29N526788 (S.M.M.), NIH Grants HL13851, AGG08377, RR04865 as well as the generous support of
PY - 1992/12/14
Y1 - 1992/12/14
N2 - 3N-(2′-[18F]Fluoroethyl)benperidol ([18F]FEB) an 18F-labeled analogue of the D2 antagonist benperidol, was evaluated as a tracer for positron emission tomography (PET). PET imaging of a living baboon showed that the fluorinated ligand rapidly localized in vivo within D2 receptor-rich brain tissue, with selective retention lasting over 2 h after tracer injection. Pretreatment of the animal with unlabeled D2-specific antagonist eticlopride (4 mg/kg, i.v.) 1 h before [18F]FEB completely abolished the selective disposition of the radioligand, whereas the regional cerebral blood flow, blood volume and peripheral metabolism/protein binding of [18F]FEB were not changed. Tracer localization when the baboon was pretreated with unlabeled ketanserin (0.55 mg/kg, i.v.) or SCH 23390 (1.1 mg/kg, i.v.) was identical to that for the control case, indicating that the [18F]FEB did not bind to S2 of D1 receptors in vivo. [18F]FEB has advantages compared to previously used PET tracers, and may be an excellent radioligand for non-invasive study of D2 receptor binding.
AB - 3N-(2′-[18F]Fluoroethyl)benperidol ([18F]FEB) an 18F-labeled analogue of the D2 antagonist benperidol, was evaluated as a tracer for positron emission tomography (PET). PET imaging of a living baboon showed that the fluorinated ligand rapidly localized in vivo within D2 receptor-rich brain tissue, with selective retention lasting over 2 h after tracer injection. Pretreatment of the animal with unlabeled D2-specific antagonist eticlopride (4 mg/kg, i.v.) 1 h before [18F]FEB completely abolished the selective disposition of the radioligand, whereas the regional cerebral blood flow, blood volume and peripheral metabolism/protein binding of [18F]FEB were not changed. Tracer localization when the baboon was pretreated with unlabeled ketanserin (0.55 mg/kg, i.v.) or SCH 23390 (1.1 mg/kg, i.v.) was identical to that for the control case, indicating that the [18F]FEB did not bind to S2 of D1 receptors in vivo. [18F]FEB has advantages compared to previously used PET tracers, and may be an excellent radioligand for non-invasive study of D2 receptor binding.
KW - 3N-(2′-[F]Fluoroethyl)benperidol
KW - D receptor
KW - Dopamine
KW - Imaging
KW - Neurotransmitter receptor
KW - Positron emission tomography
KW - Receptor binding
UR - http://www.scopus.com/inward/record.url?scp=0026619877&partnerID=8YFLogxK
U2 - 10.1016/0304-3940(92)90813-M
DO - 10.1016/0304-3940(92)90813-M
M3 - Article
C2 - 1300511
AN - SCOPUS:0026619877
SN - 0304-3940
VL - 148
SP - 97
EP - 100
JO - Neuroscience Letters
JF - Neuroscience Letters
IS - 1-2
ER -