Volicer L, Biagioni T M
J Neurochem. 1982 Feb;38(2):591-3. doi: 10.1111/j.1471-4159.1982.tb08668.x.
Characteristics of receptor binding of diazepam and flunitrazepam in three brain areas were compared. It was found that in the cerebral cortex and cerebellum the number of sites was similar for both ligands and that the affinity of diazepam was four times lower than the affinity of flunitrazepam. In contrast, when binding in the hippocampus was analyzed (assuming the presence of homogeneous binding sites), it was found that the number of binding sites was higher and that the affinity was 17 times lower for diazepam than for flunitrazepam. This difference is due to the presence of two diazepam binding sites in this brain area, as demonstrated by a Scatchard analysis.
比较了地西泮和氟硝西泮在三个脑区的受体结合特征。结果发现,在大脑皮层和小脑中,两种配体的结合位点数量相似,且地西泮的亲和力比氟硝西泮低四倍。相比之下,当分析海马体中的结合情况时(假设存在均匀的结合位点),发现结合位点数量更多,且地西泮的亲和力比氟硝西泮低17倍。如Scatchard分析所示,这种差异是由于该脑区存在两个地西泮结合位点。