Matches in SemOpenAlex for { <https://semopenalex.org/work/W2279693890> ?p ?o ?g. }
Showing items 1 to 74 of
74
with 100 items per page.
- W2279693890 endingPage "1612" @default.
- W2279693890 startingPage "1612" @default.
- W2279693890 abstract "1612 Objectives The monoamine oxidase A (MAO-A) is responsible for the oxidation of amines from endogenous and exogenous sources. Main substrates are serotonin, dopamine and norepinephrine. Several 11C-labeled MAO-A inhibitors for molecular imaging have been developed, e.g. [11C]harmine has been already used in animal or competition studies in humans. To overcome the limitation of carbon-11, with its half-life of 20.3 min Blom and co-workers synthesized 18F-labeled harmine derivatives and investigated the in vitro behavior. Our aim was to investigate the in vivo behavior of these compounds. Methods The fluorine-18 labeling of the precursors was performed at the hydroxyl group of harmol. Whilst three of the compounds also contained PEG-spacers of different length and a tosyl group for 18F-direct fluorination, the fourth compound was synthesized via 18F-fluoroethylation of harmol and all were evaluated in µPET studies. Results We synthesized four 18F-fluorinated radiotracers, three via direct labeling and one via labeling with 2-[18F]fluoroethyl tosylate. After optimization of the reaction conditions radiochemical yields (RCY) of 30-45% in case of the direct labeling and 80% in case of the labeling with the prosthetic group were obtained. The in vivo behavior of all compounds was examined in µPET studies with rats, which showed that the pegylated compounds did not cross the Blood Brain Barrier (BBB). Thereforere blocking studies with the superior compound were performed to determine the specificity, which showed a high specificity and also allowed the visualization of MAO-A rich regions like nucleolus coeruleus or thalamus. Conclusions Four harmine derivatives were labeled with fluorine-18 and their RCY increased by using a µwave-supported synthesis during direct labeling. µPET studies in rats were performed with all compounds, revealing that only the 18F-fluorethylated compound was able to cross the BBB and blocking experiments with the 18F-fluorethylated compound were done, which showed a high MAO-A selectivity" @default.
- W2279693890 created "2016-06-24" @default.
- W2279693890 creator A5003391696 @default.
- W2279693890 creator A5014835551 @default.
- W2279693890 creator A5037619007 @default.
- W2279693890 creator A5076225067 @default.
- W2279693890 date "2012-05-01" @default.
- W2279693890 modified "2023-10-01" @default.
- W2279693890 title "In vivo evaluation of pegylated [18F]harmine derivatives: Selective reversible MAO-A inhibitors" @default.
- W2279693890 hasPublicationYear "2012" @default.
- W2279693890 type Work @default.
- W2279693890 sameAs 2279693890 @default.
- W2279693890 citedByCount "0" @default.
- W2279693890 crossrefType "journal-article" @default.
- W2279693890 hasAuthorship W2279693890A5003391696 @default.
- W2279693890 hasAuthorship W2279693890A5014835551 @default.
- W2279693890 hasAuthorship W2279693890A5037619007 @default.
- W2279693890 hasAuthorship W2279693890A5076225067 @default.
- W2279693890 hasConcept C114461151 @default.
- W2279693890 hasConcept C150903083 @default.
- W2279693890 hasConcept C170493617 @default.
- W2279693890 hasConcept C181199279 @default.
- W2279693890 hasConcept C185592680 @default.
- W2279693890 hasConcept C207001950 @default.
- W2279693890 hasConcept C2775864247 @default.
- W2279693890 hasConcept C2776024655 @default.
- W2279693890 hasConcept C2781450507 @default.
- W2279693890 hasConcept C55493867 @default.
- W2279693890 hasConcept C71924100 @default.
- W2279693890 hasConcept C86803240 @default.
- W2279693890 hasConcept C98274493 @default.
- W2279693890 hasConceptScore W2279693890C114461151 @default.
- W2279693890 hasConceptScore W2279693890C150903083 @default.
- W2279693890 hasConceptScore W2279693890C170493617 @default.
- W2279693890 hasConceptScore W2279693890C181199279 @default.
- W2279693890 hasConceptScore W2279693890C185592680 @default.
- W2279693890 hasConceptScore W2279693890C207001950 @default.
- W2279693890 hasConceptScore W2279693890C2775864247 @default.
- W2279693890 hasConceptScore W2279693890C2776024655 @default.
- W2279693890 hasConceptScore W2279693890C2781450507 @default.
- W2279693890 hasConceptScore W2279693890C55493867 @default.
- W2279693890 hasConceptScore W2279693890C71924100 @default.
- W2279693890 hasConceptScore W2279693890C86803240 @default.
- W2279693890 hasConceptScore W2279693890C98274493 @default.
- W2279693890 hasLocation W22796938901 @default.
- W2279693890 hasOpenAccess W2279693890 @default.
- W2279693890 hasPrimaryLocation W22796938901 @default.
- W2279693890 hasRelatedWork W1541819110 @default.
- W2279693890 hasRelatedWork W2005329402 @default.
- W2279693890 hasRelatedWork W2010946110 @default.
- W2279693890 hasRelatedWork W2012876772 @default.
- W2279693890 hasRelatedWork W2019519553 @default.
- W2279693890 hasRelatedWork W2064268133 @default.
- W2279693890 hasRelatedWork W2100250530 @default.
- W2279693890 hasRelatedWork W2159496474 @default.
- W2279693890 hasRelatedWork W2189692100 @default.
- W2279693890 hasRelatedWork W2257502804 @default.
- W2279693890 hasRelatedWork W2288138403 @default.
- W2279693890 hasRelatedWork W2477646067 @default.
- W2279693890 hasRelatedWork W2583644044 @default.
- W2279693890 hasRelatedWork W2607931808 @default.
- W2279693890 hasRelatedWork W2748825950 @default.
- W2279693890 hasRelatedWork W2883108221 @default.
- W2279693890 hasRelatedWork W2952173343 @default.
- W2279693890 hasRelatedWork W2952685537 @default.
- W2279693890 hasRelatedWork W3111742328 @default.
- W2279693890 hasRelatedWork W3164277317 @default.
- W2279693890 hasVolume "53" @default.
- W2279693890 isParatext "false" @default.
- W2279693890 isRetracted "false" @default.
- W2279693890 magId "2279693890" @default.
- W2279693890 workType "article" @default.