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.

Article date: 1990/5/1

PubMed ID: 2171544

Journal name: Farmaco (Societa chimica italiana : 1989) (ISSN: 0014-827X)


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.

Author List: Nacci V, Fiorini I, Garofalo A, Cagnotto A

Publication Types: Journal Article; Research Support, Non-U.S. Gov't

Substances mentioned in the article: Psychotropic Drugs; Pyrroles; Receptors, GABA-A; Thiazepines; 7-acetoxy-6,7-dihydro-6-(4-methoxyphenyl)pyrrolo(2,1-d)(1,5)benzothiazepine; 6-(4-methoxyphenyl)pyrrolo(2,1-d)(1,5)benzothiazepin-7(6H)-ol;

Mesh terms: Animals; Binding, Competitive/drug effects; Brain Chemistry/drug effects; Chemical Phenomena; Chemistry; In Vitro Techniques; Male; Psychotropic Drugs/chemical synthesis; Pyrroles/chemical synthesis; Rats; Rats, Inbred Strains; Receptors, GABA-A/drug effects; Synaptic Membranes/metabolism; Thiazepines/chemical synthesis;

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