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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Binding, Competitive / drug effects
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Brain Chemistry / drug effects
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Chemical Phenomena
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Chemistry
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In Vitro Techniques
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Male
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Psychotropic Drugs / chemical synthesis*
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Pyrroles / chemical synthesis*
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Pyrroles / metabolism
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Pyrroles / pharmacology
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Rats
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Rats, Inbred Strains
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Receptors, GABA-A / drug effects
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Receptors, GABA-A / metabolism*
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Synaptic Membranes / metabolism
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Thiazepines / chemical synthesis*
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Thiazepines / metabolism
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Thiazepines / pharmacology
Substances
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Psychotropic Drugs
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Pyrroles
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Receptors, GABA-A
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Thiazepines
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7-acetoxy-6,7-dihydro-6-(4-methoxyphenyl)pyrrolo(2,1-d)(1,5)benzothiazepine
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6-(4-methoxyphenyl)pyrrolo(2,1-d)(1,5)benzothiazepin-7(6H)-ol