In the present study, we have synthesized and tested novel pyridopyrrolo- and pyrrolobenzoxazepine derivatives, as novel and selective peripheral type benzodiazepine receptor (PBR) ligands, and their ability to modulate steroid biosynthesis has been investigated. A subset of new ligands bind the PBR (rat brain and testis) with picomolar affinity, representing the most potent ligands that have been identified to date: and elicited effects on endogenous rate of steroidogenesis in MA10 Leydig cells, having similar potency and effect as PK11195. Several compounds, differently substituted at C-7, were used as molecular yardsticks to probe the spatial dimension of the lipophilic pocket L4 in the receptor binding site.
Campiani, G., Ramunno, A., Fiorini, I., Nacci, V., Morelli, E., Novellino, E., et al. (2002). Synthesis of new molecular probes for investigation of steroid biosynthesis induced by selective interaction with peripheral-type benzodiazepine receptors (PBR). JOURNAL OF MEDICINAL CHEMISTRY, 45(19), 4276-4281 [10.1021/jm020849l].
Synthesis of new molecular probes for investigation of steroid biosynthesis induced by selective interaction with peripheral-type benzodiazepine receptors (PBR)
Campiani, G.;Fiorini, I.;Nacci, V.;
2002-01-01
Abstract
In the present study, we have synthesized and tested novel pyridopyrrolo- and pyrrolobenzoxazepine derivatives, as novel and selective peripheral type benzodiazepine receptor (PBR) ligands, and their ability to modulate steroid biosynthesis has been investigated. A subset of new ligands bind the PBR (rat brain and testis) with picomolar affinity, representing the most potent ligands that have been identified to date: and elicited effects on endogenous rate of steroidogenesis in MA10 Leydig cells, having similar potency and effect as PK11195. Several compounds, differently substituted at C-7, were used as molecular yardsticks to probe the spatial dimension of the lipophilic pocket L4 in the receptor binding site.File | Dimensione | Formato | |
---|---|---|---|
jm020849l.pdf
non disponibili
Tipologia:
PDF editoriale
Licenza:
NON PUBBLICO - Accesso privato/ristretto
Dimensione
80.94 kB
Formato
Adobe PDF
|
80.94 kB | Adobe PDF | Visualizza/Apri Richiedi una copia |
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
https://hdl.handle.net/11365/19471
Attenzione
Attenzione! I dati visualizzati non sono stati sottoposti a validazione da parte dell'ateneo