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[Relationship between the structure, affinity to benzodiazepine receptors and properties of 5-halogenophenyl-1,2-dihydro-3H-1,4- benzodiazepine-2-ones].

作者信息

Andronati S A, Chepelev V M, Iakubovskaia L N, Val'dman A V, Voronina T A

出版信息

Bioorg Khim. 1983 Oct;9(10):1357-61.

PMID:6091687
Abstract

The inhibition constants of [3H] diazepam specific binding with benzodiazepine receptor by 7-bromo-5-halogenophenyl-1,2-dihydro-3H-1,4-benzodiazepines change symbatically with molar extinctions of the longwave maxima in UV spectra, the basicity of these compounds and activity by the assays of antagonism with pentilentetrazol, the potentiation of hexenal sleep and disturbance of orientation reflexes. It has been suggested that anxiolytic, hypnosedative and antipentilentetrazol effects, and to lesser extent anticonvulsive and myorelaxant effects, of benzodiazepines and determined by affinity for benzodiazepine receptors.

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