Fiorenza, Dario (2022) Sintesi automatizzata del nuovo ligando per TSPO PET imaging [18F]Fluoroetiltemazepam e metodologia di nanoincapsulazione in matrici lipidiche. [Tesi di dottorato]
Preview |
Text
Fiorenza_Dario_35.pdf Download (1MB) | Preview |
| Item Type: | Tesi di dottorato |
|---|---|
| Resource language: | Italiano |
| Title: | Sintesi automatizzata del nuovo ligando per TSPO PET imaging [18F]Fluoroetiltemazepam e metodologia di nanoincapsulazione in matrici lipidiche |
| Creators: | Creators Email Fiorenza, Dario dario.fiorenza@unina.it |
| Date: | 1 December 2022 |
| Number of Pages: | 85 |
| Institution: | Università degli Studi di Napoli Federico II |
| Department: | Scienze Biomediche Avanzate |
| Dottorato: | Scienze biomorfologiche e chirurgiche |
| Ciclo di dottorato: | 35 |
| Coordinatore del Corso di dottorato: | nome email Cuocolo, Alberto cuocolo@unina.it |
| Tutor: | nome email del Vecchio, Silvana UNSPECIFIED Salvatore, Marco UNSPECIFIED |
| Date: | 1 December 2022 |
| Number of Pages: | 85 |
| Keywords: | translocator protein, benzodiazepine, neuroinflammation |
| Settori scientifico-disciplinari del MIUR: | Area 06 - Scienze mediche > MED/36 - Diagnostica per immagini e radioterapia |
| Date Deposited: | 16 Dec 2022 18:21 |
| Last Modified: | 09 Apr 2025 13:33 |
| URI: | http://www.fedoa.unina.it/id/eprint/14706 |
Collection description
Benzodiazepines, including temazepam are described as TSPO antagonists. In fact, TSPO was initially described as a peripheral benzodiazepine receptor (PBR) with a secondary binding site for diazepam. TSPO is a potential imaging target of neuroinflammation because there is an amplification of the expression of this receptor. Herein, we developed a novel fluorinated benzodiazepine ligand, [18F]Fluoroethyltemazepam ([18F]F-FETEM), for positron emission tomography (PET) imaging of translocator protein (18 kDa). [18F]F-FETEM was radiolabelled with an automated synthesizer via a one-pot procedure. We conducted a [18F]F-aliphatic nucleophilic substitution of a tosylated precursor followed by purification on C18 and Alumina N SPE cartridges. Quality control tests was also carried out. We obtained 2.0–3.0% decay-uncorrected radiochemical activity yield (3.7% decay-corrected) within the whole synthesis time about 33 min. The radiochemical purity of [18F]F-FETEM was over 90% by TLC analysis. This automated procedure may be used as basis for future production of [18F]F-FETEM for preclinical PET imaging studies. As regards the possible methodology of encapsulation of [18F]-fluoroethyltemazepam radioligand in nanocarriers, a strategy of functionalization of complex lipid derivatives of phosphoethanolamine, whose polar head containing the -NH2 group can react with the FDG forming a Amadori product not complete, through a Maillard reaction. The compound synthesized according to this reaction scheme, which constitutes the external skeleton of the self-assembling nanocarrier, is FDG-18: 1 Caproylamina PE.
Downloads
Downloads per month over past year
Actions (login required)
 |
View Item |
