Improved synthesis of [¹8F]FS-PTAD as a new tyrosine-specific prosthetic group for radiofluorination of biomolecules.
Appl Radiat Isot
; 104: 136-42, 2015 Oct.
Article
en En
| MEDLINE
| ID: mdl-26159662
ABSTRACT
A novel prosthetic group, 4-(p-([(18)F]fluorosulfonyl)phenyl)-1,2,4-triazoline-3,5-dione ([(18)F]FS-PTAD) for site-specific radiofluorination of tyrosine residue in small molecules is described. Coupling of [(18)F]FS-PTAD with L-tyrosine, N-acetyl-L-tyrosine methyl amide and phenol as model compounds were achieved in buffered aqueous solution at room temperature, resulting in the corresponding fluorinated tyrosine and phenol derivatives. The total synthesis time including radiosynthesis, HPLC purification and formulation was less than 60 min (n=15) with ≥98% radio chemical purity. An initial in vitro evaluation of [(18)F]FS-PTAD-tyrosine in glioma cell lines revealed moderate uptake.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Tirosina
/
Radioisótopos de Flúor
/
Glioma
/
Marcaje Isotópico
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Appl Radiat Isot
Asunto de la revista:
MEDICINA NUCLEAR
/
SAUDE AMBIENTAL
Año:
2015
Tipo del documento:
Article
País de afiliación:
Alemania