A number of new pyrrolobenzothiazepine derivatives and a pyrrolobenzothiazocine derivative have been synthesized and evaluated for their affinity towards the 'peripheral-type' benzodiazepine receptor (PER). The new compounds were tested in rat cortex, a tissue expressing a high density of mitochondrial PER. Some of the pyrrolobenzothiazepines exhibited IC50 values in the low nanomolar range as measured by the displacement of [H-3]PK 11195 binding. Compound 4i was found to be the most potent ligand for this receptor in the pyrrolobenzothiazepine subgroup with an IC50 practically identical to that determined for PK 11195. Structure-affinity relationships (SARs) have been developed to elucidate the topology of the PER binding site.

Campiani, G., Nacci, V., Fiorini, I., De Filippis, M.P., Garofalo, A., Ciani, S.M., et al. (1997). New pyrrolobenzothiazepine derivatives as molecular probes of the ‘peripheral-type’ benzodiazepine receptor (PBR) binding site. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 32(3), 241-251 [10.1016/S0223-5234(97)83975-X].

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

Campiani G.;Nacci V.;Fiorini I.;
1997-01-01

Abstract

A number of new pyrrolobenzothiazepine derivatives and a pyrrolobenzothiazocine derivative have been synthesized and evaluated for their affinity towards the 'peripheral-type' benzodiazepine receptor (PER). The new compounds were tested in rat cortex, a tissue expressing a high density of mitochondrial PER. Some of the pyrrolobenzothiazepines exhibited IC50 values in the low nanomolar range as measured by the displacement of [H-3]PK 11195 binding. Compound 4i was found to be the most potent ligand for this receptor in the pyrrolobenzothiazepine subgroup with an IC50 practically identical to that determined for PK 11195. Structure-affinity relationships (SARs) have been developed to elucidate the topology of the PER binding site.
1997
Campiani, G., Nacci, V., Fiorini, I., De Filippis, M.P., Garofalo, A., Ciani, S.M., et al. (1997). New pyrrolobenzothiazepine derivatives as molecular probes of the ‘peripheral-type’ benzodiazepine receptor (PBR) binding site. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 32(3), 241-251 [10.1016/S0223-5234(97)83975-X].
File in questo prodotto:
File Dimensione Formato  
EurJMedChem_1997.pdf

non disponibili

Tipologia: Post-print
Licenza: NON PUBBLICO - Accesso privato/ristretto
Dimensione 2.28 MB
Formato Adobe PDF
2.28 MB Adobe PDF   Visualizza/Apri   Richiedi una copia

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11365/31416
 Attenzione

Attenzione! I dati visualizzati non sono stati sottoposti a validazione da parte dell'ateneo