Abstract

1-Cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine 1 (PB28) and 2- Methoxy-5-methyl-N-[4-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)butyl]benzamide 2 (RHM-1) represent leads for tumor diagnosis, given their high affinity at sigma2 receptors. With the purpose of obtaining good candidates for s2 PET tracers development, hybrid structures between 1 and 2 were designed. Excellent sigma1/sigma2 selectivities were reached when 6,7-dimethoxytetrahydroisoquinolinewas linked to an omethoxy substituted arylamide (11a, 12a, 15a), and for these benzamides an intramolecular H-bond in the active conformation at the s sites, was hypothesized. However these excellent s2 ligands were accompanied by interaction with P-gp, which may limit their use as sigma2 receptor PET agents when tumors overexpress P-gp. Compound 15a whose P-gp interaction was just moderate represents an interesting tool for the development of sigma2 PET tracers useful in tumors overexpressing P-gp.

Autore Pugliese

• Abate Carmen , Berardi Francesco , Contino Marialessandra , Colabufo Nicola Antonio , Ferorelli Savina

Tutti gli autori

• ABATE C.;BERARDI F.;CONTINO M.;COLABUFO N.A.;PERRONE R.;FERORELLI S.

Titolo volume/Rivista

Non Disponibile

Anno di pubblicazione

2011

ISSN

0223-5234

ISBN

Non Disponibile

Numero di citazioni Wos

20

Ultimo Aggiornamento Citazioni

Non Disponibile

Numero di citazioni Scopus

19

Ultimo Aggiornamento Citazioni

Non Disponibile

Settori ERC

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Codici ASJC

Non Disponibile