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|Title:||Synthesis of new molecular probes for investigation of steroid biosynthesis induced by selective interaction with peripheral-type benzodiazepine receptors (PBR)||Authors:||Campiani, Giuseppe
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.
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