ArticleNuclear medicine and biology2008
2-(2'-((Dimethylamino)methyl)-4'-(3-[(18)F]fluoropropoxy)-phenylthio)benzenamine for positron emission tomography imaging of serotonin transporters.
Article in Nuclear medicine and biology, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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8 citing papers in PubMed, 27 citations in OpenAlex.
- Toxicity and radiation dosimetry studies of the serotonin transporter radioligand [(18) F]AFM in rats and monkeys.EJNMMI research · 2014Article
- PET imaging of the brain serotonin transporters (SERT) with N,N-dimethyl-2-(2-amino-4-[18F]fluorophenylthio)benzylamine (4-[18F]-ADAM) in humans: a preliminary study.European journal of nuclear medicine and molecular imaging · 2013Article
- Synthesis and evaluation of novel N-fluoropyridyl derivatives of tropane as potential PET imaging agents for the dopamine transporter.Bioorganic & medicinal chemistry letters · 2011Article
- Synthesis, fluorine-18 radiolabeling, and biological evaluation of N-((E)-4-fluorobut-2-en-1-yl)-2beta-carbomethoxy-3beta-(4'-halophenyl)nortropanes: candidate radioligands for in vivo imaging of the brain dopamine transporter with positron emission tomography.Journal of medicinal chemistry · 2010Article
- In vivo studies of the SERT-selective [18F]FPBM and VMAT2-selective [18F]AV-133 radiotracers in a rat model of Parkinson's disease.Nuclear medicine and biology · 2010Article
- Biodistribution, toxicity and radiation dosimetry studies of the serotonin transporter radioligand 4-[18F]-ADAM in rats and monkeys.European journal of nuclear medicine and molecular imaging · 2010Article
- Fluorine-18 Radiolabeled PET Tracers for Imaging Monoamine Transporters: Dopamine, Serotonin, and Norepinephrine.PET clinics · 2009Article
- 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.Journal of medicinal chemistry · 2008Article
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6 authors at 1 institution in 1 country.
Funding
Abstract
introductionA new (18)F ligand, 2-(2'-((dimethylamino)methyl)-4'-(3-[(18)F]fluoropropoxy)-phenylthio)benzenamine ([(18)F]1), for positron emission tomography (PET) imaging of serotonin transporters (SERT) was evaluated.
methodsBinding affinity was determined through in vitro binding assays with LLC-PK1 cells overexpressing SERT, NET or DAT (LLC-SERT, LLC-NET and LLC-DAT) and with rat cortical homogenates. Localization and selectivity of [(18)F]1 binding in vivo were evaluated by biodistribution, autoradiography and A-PET imaging studies in rats.
resultsThis compound displayed excellent binding affinity for SERT in vitro with K(i)=0.33 and 0.24 nM in LLC-SERT and rat cortical homogenates, respectively. Biodistribution studies with [(18)F]1 showed good brain uptake (1.61% dose/g at 2 min postinjection), high uptake into the hypothalamus (1.22% dose/g at 30 min) and a high target-to-nontarget (hypothalamus to cerebellum) ratio of 9.66 at 180 min postinjection. Pretreatment with a SERT selective inhibitor considerably inhibited [(18)F]1 binding in biodistribution studies. Ex vivo autoradiography reveals [(18)F]1 localization to brain regions with high SERT density, and this binding was blocked by pretreatment with SERT selective inhibitors. Small animal PET (A-PET) imaging in rats provided clear images of tracer localization in the thalamus, midbrain and striatum. In A-PET chasing experiments, injecting a SERT selective inhibitor 75 min post-tracer injection causes a dramatic reduction in regional radioactivity and the target-to-nontarget ratio.
conclusionThe results of the biological studies and the ease of radiosynthesis with moderately good radiochemical yield (RCY=10-35%) make [(18)F]1 an excellent candidate for SERT PET imaging.
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