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Abstract [3 H] Flunitrazepam was used to characterize benzodiazepine binding sites in human brain. The benzodiazepine binding sites exhibited high affinity, pharmacological specificity and saturability in their binding of [3 H] flunitrazepam. The dissociation constant (K D) of [3 H] flunitrazepam binding was determined by three different methods and found to be in the range of 2–3 nM. The potency of several benzodiazepine analogs to inhibit specific [3 H]-flunitrazepam binding in vitro correlated well with their potency in several in vivo human and animal tests. The density of [3 H]-flunitrazepam binding sites was highest in the cerebrocortical and rhinencephalic areas, intermediate in the cerebellum, and lowest in the brain stem and commissural tracts.