Research on compounds with psychotropic activity IX - synthesis of 6-p-methoxyphenylpyrrolo[2,1-d][1,5]benzothiazepines and evaluation of their affinities for BDZ and GABA receptor subtypes

V. Nacci, I. Fiorini, A. Garofalo, A. Cagnotto

Research output: Contribution to journalArticle

Abstract

6-p-Methoxyphenylpyrrolo[2,1-d][1,5]benzothiazepin-7(6H)-one (IV), cis-7-acetoxy-6,7-dihydro-6-p-methoxyphenylpyrrolo[2,1- d][1,5]benzothiazepine (V) and some significant 7-acyloxy-6-p-methoxyphenylpyrrolo[2,1- d][1,5]benzothiazepines (VI a-g) were synthesized and tested in vitro for inhibition of the specific binding of 3H-Flunitrazepam, 3H-PK 11195, 3H-Muscimol and 3H-(-)Baclofen to central and peripheral benzodiazepine, GABA-A and GABA-B receptors, respectively. The compounds (IV), (VI a) and (VI c) were active on the peripheral benzodiazepine receptor; in particular (VI a) and (VI c) were very active. The compound (VI g) showed an affinity, even though scanty, for the central benzodiazepine receptor.

Original languageEnglish
Pages (from-to)545-557
Number of pages13
JournalFarmaco
Volume45
Issue number5
Publication statusPublished - 1990

ASJC Scopus subject areas

  • Drug Discovery
  • Pharmaceutical Science

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