Relationship between the structure, affinity to benzodiazepine receptors and properties of 5-halogenophenyl-1,2-dihydro-3H-1,4- benzodiazepine-2-ones
Andronati, S.A.; Chepelev, V.M.; Iakubovskaia, L.N.; Val'dman, A.V.; Voronina, T.A.
Bioorganicheskaia Khimiia 9(10): 1357-1361
1983
ISSN/ISBN: 0132-3423 PMID: 6091687 Document Number: 215294
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.