Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12779/4671
Title: Synthesis of new molecular probes for investigation of steroid biosynthesis induced by selective interaction with peripheral-type benzodiazepine receptors (PBR)
Authors: Campiani, Giuseppe 
Ramunno, A.
Fiorini, I.
Nacci, V.
Morelli, E.
Novellino, E.
Goegan, M.
Mennini, T.
Sullivan, S.
Zisterer, D. M.
Williams, C. D.
Issue Date: 2002
Project: None 
Journal: JOURNAL OF MEDICINAL CHEMISTRY
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.
Description: 
36646
URI: http://hdl.handle.net/20.500.12779/4671
ISSN: 0022-2623
DOI: 10.1021/jm020849l
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