Asymmetric Tc-Nitrido Complexes for Imaging 5HT1A Receptor
| Autor: | Bolzati C., Mahmood A., Malagò E., Boschi A., Uccelli L., Friebe M., Jones A., Duatti A. |
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| Jazyk: | angličtina |
| Rok vydání: | 2002 |
| Předmět: | |
| Zdroj: | Sixth International Symposium on Technetium in Chemistry and Nuclear Medicine, pp. 369–374, Bressanone (Bz) IT, September 4-7, 2002 info:cnr-pdr/source/autori:Bolzati C.; Mahmood A.; Malagò E.; Boschi A.; Uccelli L.; Friebe M.; Jones A.; Duatti A./congresso_nome:Sixth International Symposium on Technetium in Chemistry and Nuclear Medicine/congresso_luogo:Bressanone (Bz) IT/congresso_data:September 4-7, 2002/anno:2002/pagina_da:369/pagina_a:374/intervallo_pagine:369–374 |
| Popis: | The [TcN(PNP)]2+ metal fragment allows the incorporation of a bioactive molecule into a 99mTc-nitrido complex. Herein we describe the first application of this procedure to a 2-methoxyphenyl piperazine (2-MPP) pharmacophore, wich display preferential affinity for the 5HT1A receptors. An N-derivatized cysteine, namely 2-MPPP-cys-OS, where 2-MPPP is 3-[4-(2-methoxyphenyl)piperazin-1-yl]propionate was synthetized as the pharmacophore containing bifunctional-ligand. The asimmetric Tc(V)-nitrido complexes [99g/99m Tc(N)(PNP)(2-MPPP-cys-OS)] (PNP= PNP3, PNP4), were obtained in hig yields (95%), by simultaneous addition of PNP and 2.MPPP-cys-OS ligands to a solution containing a 99mTc-nitrido precursor. Biological evaluation of the complexes were performed by conducting in vitro 5HT1A receptor-binding assays and in vivo biodistribution studies in rats. |
| Databáze: | OpenAIRE |
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