TY - JOUR
T1 - Central serotonergic S2 binding in Papio anubis measured in vivo with N-ω-[18F]fluoroethylketanserin and PET
AU - Moerlein, Stephen M.
AU - Perlmutter, Joel S.
N1 - Funding Information:
We are grateful for the support of all the members of the Division of Radiation Sciences at the Mallinckrodt Institute of Radiology. This work was supported by the McDonnell Center for the Study of Higher Brain Function, NIH FIRST Award I R29NS26788, NIH Grants
PY - 1991/2/11
Y1 - 1991/2/11
N2 - N-ω-[18F]fluoroethylketanserin ([18F]FEK), an 18F-labeled analogue of the serotonin S2 antagonist ketanserin, was evaluated for use with positron emission tomography (PET). PET imaging of a baboon brain following injection of [18F]FEK indicated that the fluorinated ligand rapidly localized in vivo within S2 receptor-rich tissues ( frontal cortex cerebellum radioactivity ratio = 2.5 after 15 min), and selective localization was retained for as long as 3 h post injection. Pretreatment with unlabeled ketanserin (15 mg/kg, i.v.) 1 h prior to [18F]FEK completely abolished selective localization of the radiotracer, whereas regional cerebral blood flow, cerebral blood volume, and the free fraction of [18F]FEK in arterial blood were unaltered. [18F]FEK has several advantages compared to previously used PET radiopharmaceuticals, and may be an excellent radioligand for non-invasive evaluation of S2 binding in vivo.
AB - N-ω-[18F]fluoroethylketanserin ([18F]FEK), an 18F-labeled analogue of the serotonin S2 antagonist ketanserin, was evaluated for use with positron emission tomography (PET). PET imaging of a baboon brain following injection of [18F]FEK indicated that the fluorinated ligand rapidly localized in vivo within S2 receptor-rich tissues ( frontal cortex cerebellum radioactivity ratio = 2.5 after 15 min), and selective localization was retained for as long as 3 h post injection. Pretreatment with unlabeled ketanserin (15 mg/kg, i.v.) 1 h prior to [18F]FEK completely abolished selective localization of the radiotracer, whereas regional cerebral blood flow, cerebral blood volume, and the free fraction of [18F]FEK in arterial blood were unaltered. [18F]FEK has several advantages compared to previously used PET radiopharmaceuticals, and may be an excellent radioligand for non-invasive evaluation of S2 binding in vivo.
KW - Imaging
KW - Ketanserin
KW - N-ω-[F]Fluoroethylketanserin
KW - Positron emission tomography
KW - S receptor
KW - Serotonin
UR - http://www.scopus.com/inward/record.url?scp=0025925030&partnerID=8YFLogxK
U2 - 10.1016/0304-3940(91)90149-N
DO - 10.1016/0304-3940(91)90149-N
M3 - Article
C2 - 2062450
AN - SCOPUS:0025925030
SN - 0304-3940
VL - 123
SP - 23
EP - 26
JO - Neuroscience Letters
JF - Neuroscience Letters
IS - 1
ER -