Synthesis and biological evaluation of new, potential MAO-B ligands.
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2019
Authors
Jevtić, Ivana
Lai, Hang
Penjišević, Jelena

Teodoro, Rodrigo

Dukic-Stefanovic, Sladjana
Brust, Peter

Kostić-Rajačić, Slađana

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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.
Keywords:
radiofluorinated ligands / positron emission tomography / monoamine oxidase-B / 1-cinnamyl-4-arylpiperazineSource:
Abstract Book - FENS regional meeting, July 10-13, 2019, Belgrade, Serbia, 2019, 286-286Publisher:
- Serbian Neuroscience Society / Društvo za neuronauke Srbije
- National Neurocience Society of Romania
- Neuroscience Society of Turkey
Funding / projects:
- DAAD (grant No.57391403)
- Structure-activity relationship of newly synthesized biological active compound (RS-172032)
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IHTMTY - 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 .