Abstract

Sigma2 Receptors are promising biomarkers for cancer diagnosis given the relationship between the proliferative status of tumors and their density. With the aim of contributing to the research of sigma2 receptor Positron Emission Tomography (PET) probes, we developed 2-[3-[6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl]propyl]-3,4-dihydroisoquinolin-1(2H)-one (3), with optimal 2 pharmacological properties and appropriate lipophilicity. Hence, 3 served as the lead compound for the development of a series of dihydroisoquinolinones amenable to radiolabeling. Radiosynthesis for compound 26, which displayed the most appropriate 2 profile, was developed and 2 specific binding for the corresponding [18F]-26 was confirmed by in vitro autoradiography on rat brain slices. Despite the excellent in vitro properties, [18F]-26 could not successfully image 2 receptors in the rat brain in vivo, maybe because of its interaction with P-gp. Nevertheless, [18F]-26 may still be worthy of further investigation for the imaging of sigma2 receptors in peripheral tumors devoid of P-gp overexpression.

Autore Pugliese

• Abate Carmen , Berardi Francesco , Niso Mauro

Tutti gli autori

• ABATE C.;BERARDI F.;NISO M.;PERRONE R.

Titolo volume/Rivista

Non Disponibile

Anno di pubblicazione

2013

ISSN

0223-5234

ISBN

Non Disponibile

Numero di citazioni Wos

21

Ultimo Aggiornamento Citazioni

Non Disponibile

Numero di citazioni Scopus

20

Ultimo Aggiornamento Citazioni

Non Disponibile

Settori ERC

Non Disponibile

Codici ASJC

Non Disponibile