Preparation and first 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 first 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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Abstract

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]2þ (M¼99mTc, 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]2þ 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]2þ 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 highyield 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: Medical and Health Sciences > Health biotechnology
Medical and Health Sciences > Health sciences
Divisions: Faculty of Medical Science
Depositing User: Emilija Janevik
Date Deposited: 26 Nov 2014 10:18
Last Modified: 26 Nov 2014 10:18
URI: http://eprints.ugd.edu.mk/id/eprint/11459

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