Central serotonergic S2 binding in Papio anubis measured in vivo with N-omega-[18F]fluoroethylketanserin and PET.

Abstract:

:N-omega-[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.

journal_name

Neurosci Lett

journal_title

Neuroscience letters

authors

Moerlein SM,Perlmutter JS

doi

10.1016/0304-3940(91)90149-n

subject

Has Abstract

pub_date

1991-02-11 00:00:00

pages

23-6

issue

1

eissn

0304-3940

issn

1872-7972

pii

0304-3940(91)90149-N

journal_volume

123

pub_type

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