New pyrrolobenzothiazepine derivatives as molecular probes of the 'peripheral-type'benzodiazepine receptor (PBR) binding site

G Campiani, V Nacci, I Fiorini, MP De Filippis…

文献索引：Campiani; Nacci; Fiorini; De Filippis, Mp; Garofalo; Ciani; Greco; Novellino; Manzoni; Mennini European Journal of Medicinal Chemistry, 1997 , vol. 32, # 3 p. 241 - 251

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被引用次数: 22

摘要

A number of new pyrrolobenzothiazepine derivatives and a pyrrolobenzothiazocine derivative have been synthesized and evaluated for their affinity towards the 'peripheral- type'benzodiazepine receptor (PBR). The new compounds were tested in rat cortex, a tissue expressing a high density of mitochondrial PBR. Some of the pyrrolobenzothiazepines exhibited IC50 values in the low nanomolar range as measured by the displacement of [ ...