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.
TY - CONF
AU - Jevtić, Ivana
AU - Lai, Hang
AU - Penjišević, Jelena
AU - Teodoro, Rodrigo
AU - Dukic-Stefanovic, Sladjana
AU - Brust, Peter
AU - Kostić-Rajačić, Slađana
PY - 2019
UR - https://cer.ihtm.bg.ac.rs/handle/123456789/5836
AB - 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.
PB - Serbian Neuroscience Society / Društvo za neuronauke Srbije
PB - National Neurocience Society of Romania
PB - Neuroscience Society of Turkey
C3 - Abstract Book - FENS regional meeting, July 10-13, 2019, Belgrade, Serbia
T1 - Synthesis and biological evaluation of new, potential MAO-B ligands.
SP - 286
EP - 286
UR - https://hdl.handle.net/21.15107/rcub_cer_5836
ER -
@conference{
author = "Jevtić, Ivana and Lai, Hang and Penjišević, Jelena and Teodoro, Rodrigo and Dukic-Stefanovic, Sladjana and Brust, Peter and Kostić-Rajačić, Slađana",
year = "2019",
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.",
publisher = "Serbian Neuroscience Society / Društvo za neuronauke Srbije, National Neurocience Society of Romania, Neuroscience Society of Turkey",
journal = "Abstract Book - FENS regional meeting, July 10-13, 2019, Belgrade, Serbia",
title = "Synthesis and biological evaluation of new, potential MAO-B ligands.",
pages = "286-286",
url = "https://hdl.handle.net/21.15107/rcub_cer_5836"
}
Jevtić, I., Lai, H., Penjišević, J., Teodoro, R., Dukic-Stefanovic, S., Brust, P.,& Kostić-Rajačić, S.. (2019). Synthesis and biological evaluation of new, potential MAO-B ligands.. in Abstract Book - FENS regional meeting, July 10-13, 2019, Belgrade, Serbia
Serbian Neuroscience Society / Društvo za neuronauke Srbije., 286-286.
https://hdl.handle.net/21.15107/rcub_cer_5836
Jevtić I, Lai H, Penjišević J, Teodoro R, Dukic-Stefanovic S, Brust P, Kostić-Rajačić S. Synthesis and biological evaluation of new, potential MAO-B ligands.. in Abstract Book - FENS regional meeting, July 10-13, 2019, Belgrade, Serbia. 2019;:286-286.
https://hdl.handle.net/21.15107/rcub_cer_5836 .
Jevtić, Ivana, Lai, Hang, Penjišević, Jelena, Teodoro, Rodrigo, Dukic-Stefanovic, Sladjana, Brust, Peter, Kostić-Rajačić, Slađana, "Synthesis and biological evaluation of new, potential MAO-B ligands." in Abstract Book - FENS regional meeting, July 10-13, 2019, Belgrade, Serbia (2019):286-286,
https://hdl.handle.net/21.15107/rcub_cer_5836 .
