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Synthesis and initial characterization of a reversible, selective 18F-labeled radiotracer for human butyrylcholinesteraseGentzsch, Christian ...Purpose A neuropathological hallmark of Alzheimer's disease (AD) is the presence of amyloid-[beta] (A[beta]) plaques in the brain, which are observed in a significant number of cognitively normal, ... older adults as well. In AD, butyrylcholinesterase (BChE) becomes associated with A[beta] aggregates, making it a promising target for imaging probes to support diagnosis of AD. In this study, we present the synthesis, radiochemistry, in vitro and preliminary ex and in vivo investigations of a selective, reversible BChE inhibitor as PET-tracer for evaluation as an AD diagnostic. Procedures Radiolabeling of the inhibitor was achieved by fluorination of a respective tosylated precursor using K[18F]. IC50 values of the fluorinated compound were obtained in a colorimetric assay using recombinant, human (h) BChE. Dissociation constants were determined by measuring hBChE activity in the presence of different concentrations of inhibitor. Results Radiofluorination of the tosylate precursor gave the desired radiotracer in an average radiochemical yield of 20%(+-)3 %. Identity and >95.5 % radiochemical purity were confirmed by HPLC and TLC autoradiography. The inhibitory potency determined in Ellman's assay gave an IC50 value of 118.3%(+-)19.6 nM. Dissociation constants measured in kinetic experiments revealed lower affinity of the inhibitor for binding to the acylated enzyme (K2=68.0 nM) in comparison to the free enzyme (K1=32.9 nM). Conclusions The reversibly acting, selective radiotracer is synthetically easily accessible and retains promising activity and binding potential on hBChE. Radiosynthesis with 18F labeling of tosylates was feasible in a reasonable time frame and good radiochemical yield.Vir: Molecular imaging and biology. - ISSN 1536-1632 (Vol. 23, iss. 4, 2021, str. 505-515)Vrsta gradiva - članek, sestavni delLeto - 2021Jezik - angleškiCOBISS.SI-ID - 53866243
Avtor
Gentzsch, Christian |
Chen, Xinyu |
Spatz, Philipp |
Košak, Urban |
Knez, Damijan, farmacevt |
Nose, Naoko |
Gobec, Stanislav, 1970- |
Higuchi, Takahiro |
Decker, Michael
Teme
Alzheimerjeva bolezen |
Alzheimer's disease |
enzyme inhibitor |
positron emission tomography |
biodistribution |
quaternization
Vnos na polico
Trajna povezava
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Leto | Faktor vpliva | Izdaja | Kategorija | Razvrstitev | ||||
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JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
Baze podatkov, v katerih je revija indeksirana
Ime baze podatkov | Področje | Leto |
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Povezave do osebnih bibliografij avtorjev | Povezave do podatkov o raziskovalcih v sistemu SICRIS |
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Gentzsch, Christian | |
Chen, Xinyu | |
Spatz, Philipp | |
Košak, Urban | 33908 |
Knez, Damijan, farmacevt | 36438 |
Nose, Naoko | |
Gobec, Stanislav, 1970- | 15284 |
Higuchi, Takahiro | |
Decker, Michael |
Vir: Osebne bibliografije
in: SICRIS
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