Preparation and frst biological evaluation of novel Re-188/Tc-99m peptide conjugates with substance-P

Smilkov, Katarina and Janevik-Ivanovska, Emilija and Guerrini, Remo and Pasquali, Micol and Boschi, Alessandra and Uccelli, Licia and Di Domenico, Giovanni and Duatti, Adriano (2014) Preparation and frst biological evaluation of novel Re-188/Tc-99m peptide conjugates with substance-P. Applied Radiation and Isotopes, 92. pp. 25-31. ISSN 0969-8043

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Introduction: New 188Re and 99mTc peptide conjugates with substance- P (SP) were prepared and biologically evaluated. The radiopharmaceuticals have been labelled with the [M=N]2+ (M=99mTc, 188Re) core using a combination of pi-donor tridentate and pi-acceptor monodentate ancillary ligands.
Methods: The new radiopharmaceuticals have been prepared through a two-step reaction by simultaneous addition of the tridentate and monodentate ligands to a vial containing a preformed [M=N]2+ core. The tridentate ligand was formed by linking two cysteine residues to the terminal arginine of the undecapeptide SP, whereas the monodentate ligand was a tertiary phosphine. The preparation of the corresponding Re-188 derivative required developing a more complex chemical procedure to obtain the [Re=N]2+ core in satisfactory yields. Characterization of the resulting products was obtained by chromatographic methods. Biological evaluation was performed for both Tc-99m and Re-188 derivatives by in-vitro studies on isolated cells expressing NK1-receptors. In-vivo imaging in mice was carried out using a small-animal YAP(S)PET tomograph.
Conclusion: New Tc-99m and Re-188 peptide radiopharmaceuticals with SP have been prepared in high yield and with high-specifc activity. Both Tc-99m and Re-188 peptide radioconjugates exhibit high
affnity for NK1 receptors, thus giving further evidence to the empirical rule that structurally related Tc-99m and Re-188 radiopharmaceuticals exhibit identical biological properties.

Item Type: Article
Subjects: Natural sciences > Biological sciences
Natural sciences > Chemical sciences
Medical and Health Sciences > Health biotechnology
Medical and Health Sciences > Other medical sciences
Divisions: Faculty of Medical Science
Depositing User: Katarina Smilkov
Date Deposited: 26 Nov 2014 08:35
Last Modified: 13 Mar 2015 09:17

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