Synthesis and initial biological evaluation of a novel Tc-99m radioligand as a potential agent for 5-HT1A receptor imaging
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Najoua Mejri Abdelounis
,
Nadia Malek Saied
Abstract
The synthesis, characterization and biological evaluation of N-Tolueneferrocenecarboxamide labeled with technetium-99m (99mTc-TTCC) is reported. Biological studies in Wistar rats showed the ability of 99mTc-TPCC to cross the intact blood-brain barrier. In vivo biodistribution indicated that this complex had good brain uptake (1.32% ID/g at 5 min and 0.64% ID/g at 60 min) and good retention (about 50% of the activity was retained in the brain at 60 min post-injection). Regional brain distribution study showed that hippocampus, where the 5-HT1A receptor density is high, had the highest uptake (0.73% ID/g at 5 min p.i.) and the cerebellum, where the 5-HT1A receptor density is low, had the lowest uptake (0.12% ID/gID/g at 5 min p.i.). After blocking with 8-hydroxy-2-(dipropylamino) tetralin, the uptake of hippocampus was decreased significantly from 0.73% ID/g to 0.20% ID/g at 5 min p.i., while the cerebellum had no significant decrease. This result indicates that 99mTc complex has specific binding to 5-HT1A receptor.
©2014 Walter de Gruyter Berlin/Boston
Artikel in diesem Heft
- Frontmatter
- Excitation function of (p, α) nuclear reaction on enriched 67Zn: possibility of production of 64Cu at low energy cyclotron
- Radiochemical measurement of neutron-spectrum averaged cross sections for the formation of 64Cu and 67Cu via the (n,p) reaction at a TRIGA Mark-II reactor: Feasibility of simultaneous production of the theragnostic pair 64Cu/67Cu
- A novel dipicolinamide-dicarbollide synergistic solvent system for actinide extraction
- Plutonium sorption to nanocast mesoporous carbon
- Retrieval and purification of an aged 231Pa source from its decay daughters
- Natural radioactivity measurements in agricultural soil, fertilizer and crops in some specific areas of Kingdom of Saudi Arabia
- Utilization of a novel electrochemical 90Sr/90Y generator for the preparation of 90Y-labeled RGD peptide dimer in clinically relevant dose
- Radiochemical synthesis and biological evaluation of 3-[4-(4-[18F]fluorobenzyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine as dopamine D4 receptor radioligand
- Synthesis and initial biological evaluation of a novel Tc-99m radioligand as a potential agent for 5-HT1A receptor imaging
- Clinical scale preparation and evaluation of 131I-Rituximab for Non-Hodgkin's Lymphoma
Artikel in diesem Heft
- Frontmatter
- Excitation function of (p, α) nuclear reaction on enriched 67Zn: possibility of production of 64Cu at low energy cyclotron
- Radiochemical measurement of neutron-spectrum averaged cross sections for the formation of 64Cu and 67Cu via the (n,p) reaction at a TRIGA Mark-II reactor: Feasibility of simultaneous production of the theragnostic pair 64Cu/67Cu
- A novel dipicolinamide-dicarbollide synergistic solvent system for actinide extraction
- Plutonium sorption to nanocast mesoporous carbon
- Retrieval and purification of an aged 231Pa source from its decay daughters
- Natural radioactivity measurements in agricultural soil, fertilizer and crops in some specific areas of Kingdom of Saudi Arabia
- Utilization of a novel electrochemical 90Sr/90Y generator for the preparation of 90Y-labeled RGD peptide dimer in clinically relevant dose
- Radiochemical synthesis and biological evaluation of 3-[4-(4-[18F]fluorobenzyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine as dopamine D4 receptor radioligand
- Synthesis and initial biological evaluation of a novel Tc-99m radioligand as a potential agent for 5-HT1A receptor imaging
- Clinical scale preparation and evaluation of 131I-Rituximab for Non-Hodgkin's Lymphoma
