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Synthesis and biological evaluation of new, potential MAO-B ligands.
dc.creator | Jevtić, Ivana | |
dc.creator | Lai, Hang | |
dc.creator | Penjišević, Jelena | |
dc.creator | Teodoro, Rodrigo | |
dc.creator | Dukic-Stefanovic, Sladjana | |
dc.creator | Brust, Peter | |
dc.creator | Kostić-Rajačić, Slađana | |
dc.date.accessioned | 2023-02-27T13:32:56Z | |
dc.date.available | 2023-02-27T13:32:56Z | |
dc.date.issued | 2019 | |
dc.identifier.isbn | 978-86-917255-3-2 | |
dc.identifier.uri | https://cer.ihtm.bg.ac.rs/handle/123456789/5836 | |
dc.description.abstract | The aim of this study was to develop highly specific radiofluorinated ligands for quantitative positron emission tomography (PET) imaging of monoamine oxidase-B (MAO-B) in brain. A series of 8 fluoro derivatives of 1-cinnamyl-4-arylpiperazine were synthesized by standard methods of organic synthesis. The affinity of the compounds was determined in a competitive binding assay using L-[3H] deprenyl as radioligand on rat brain homogenates. The KD of the radioligand was determined by homologous competition. An efficient, three-step procedure for the synthesis of the potential MAO-B ligands was developed. A competitive binding assay was established, using L-[3H]deprenyl as the radioligand, and rat brain membrane homogenate. The compounds were screened (three concentrations 10-9, 10-7 and 10-5) for their MAO-B affinity. We successfully synthesized a series of fluorinated MAO-B ligands. Unfortunately, their affinities toward MAO-B have proved to be rather low. To increase the affinity further modifications are needed. | sr |
dc.language.iso | en | sr |
dc.publisher | Serbian Neuroscience Society / Društvo za neuronauke Srbije | sr |
dc.publisher | National Neurocience Society of Romania | sr |
dc.publisher | Neuroscience Society of Turkey | sr |
dc.relation | DAAD (grant No.57391403) | sr |
dc.relation | info:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172032/RS// | sr |
dc.rights | restrictedAccess | sr |
dc.source | Abstract Book - FENS regional meeting, July 10-13, 2019, Belgrade, Serbia | sr |
dc.subject | radiofluorinated ligands | sr |
dc.subject | positron emission tomography | sr |
dc.subject | monoamine oxidase-B | sr |
dc.subject | 1-cinnamyl-4-arylpiperazine | sr |
dc.title | Synthesis and biological evaluation of new, potential MAO-B ligands. | sr |
dc.type | conferenceObject | sr |
dc.rights.license | ARR | sr |
dc.citation.spage | 286 | |
dc.citation.epage | 286 | |
dc.identifier.rcub | https://hdl.handle.net/21.15107/rcub_cer_5836 | |
dc.type.version | publishedVersion | sr |