ArticleJournal of medicinal chemistry2008
Synthesis, radiosynthesis, and biological evaluation of fluorine-18-labeled 2beta-carbo(fluoroalkoxy)-3beta-(3'-((Z)-2-haloethenyl)phenyl)nortropanes: candidate radioligands for in vivo imaging of the serotonin transporter with positron emission tomography.
Article in Journal of medicinal chemistry, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.
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Who cites it
5 citing papers in PubMed.
- Effects of sevoflurane anaesthesia on radioligand binding to monoamine oxidase-B in vivo.British journal of anaesthesia · 2021Article
- In vivo quantification of the [(11)C]DASB binding in the normal canine brain using positron emission tomography.BMC veterinary research · 2015Article
- Article
- Neurobiological changes mediating the effects of chronic fluoxetine on cocaine use.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2012Article
- Fluorine-18 Radiolabeled PET Tracers for Imaging Monoamine Transporters: Dopamine, Serotonin, and Norepinephrine.PET clinics · 2009Article
Corrections and comments
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Authors and funding
11 authors.
Funding
Abstract
The meta-vinylhalide fluoroalkyl ester nortropanes 1-4 were synthesized as ligands of the serotonin transporter (SERT) for use as positron emission tomography (PET) imaging agents. In vitro competition binding assays demonstrated that 1-4 have a high affinity for the SERT (K(i) values = 0.3-0.4 nM) and are selective for the SERT over the dopamine and norepinephrine transporters (DAT and NET). MicroPET imaging in anesthetized cynomolgus monkeys with [(18)F]1-[(18)F]4 demonstrated that all four tracers behave similarly with peak uptake in the SERT-rich brain regions achieved after 45-55 min, followed by a steady washout. An awake monkey study was performed with [(18)F]1, which demonstrated that the uptake of [(18)F]1 was not influenced by anesthesia. Chase studies with the SERT ligand 15 displaced [(18)F]1-[(18)F]4, but chase studies with the DAT ligand 16 did not displace [(18)F]1-[(18)F]4 thus indicating that the tracers were binding specifically to the SERT.
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Registered trials
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