[Relationship between the structure, affinity to benzodiazepine receptors and properties of 5-halogenophenyl-1,2-dihydro-3H-1,4- benzodiazepine-2-ones].
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.
D000818:Animals; D001570:Benzodiazepinones / Q000378:metabolism / Q000494:pharmacology*; D055598:Chemical Phenomena; D002621:Chemistry; D003975:Diazepam / Q000378:metabolism / Q000494:pharmacology; D008297:Male; D051379:Mice; D011869:Radioligand Assay; D051381:Rats; D011963:Receptors, GABA-A / Q000187:drug effects* / Q000378:metabolism; D013329:Structure-Activity Relationship; D013570:Synaptic Membranes / Q000187:drug effects* / Q000378:metabolism
D001570:Benzodiazepinones; D011963:Receptors, GABA-A; D003975:Diazepam
Sviaz' mezhdu strukturoĭ, srodstvom k benzdiazepinovumu retseptoru i svoĭstvami 5-galogenofenil-1,2-digidro-3 H-1,4-benzdiazepin-2-onov.