Young W S, Kuhar M J
J Pharmacol Exp Ther. 1980 Feb;212(2):337-46.
The benzodiazepine receptor was localized in rat brain with light microscopic autoradiographic methods. The binding of [3H]flunitrazepam to slide-mounted tissue sections had all of the characteristics associated with the benzodiazepine receptor. It was saturable, or a high affinity, affected by chloride ion and gamma-aminobutyric acid and showed an appropriate pharmacology. Autoradiograms were generated by the apposition of emulsion-coated coverslips. Receptor distribution showed striking variation throughout the brain and spinal cord. Some areas showing high densities include the cerebral cortex, the molecular layer of the cerebellum, parts of the limbic system, olfactory bulb and hypothalamus and substantiae gelatinosae of the spinal trigeminal nucleus and spinal cord. White matter areas showed negligible levels of receptor. These localizations show which parts of the brain are affected by benzodiazepine administration and contribute to our understanding of the mechanism of the well-known properties of the drugs such as their anxiolytic and anticonvulsant effects.
采用光学显微镜放射自显影法对大鼠脑中的苯二氮䓬受体进行定位。[³H]氟硝西泮与载玻片上的组织切片的结合具有与苯二氮䓬受体相关的所有特征。它具有饱和性，即高亲和力，受氯离子和γ-氨基丁酸影响，并表现出适当的药理学特性。通过覆盖有乳胶的盖玻片贴合产生放射自显影片。受体分布在整个脑和脊髓中显示出显著差异。一些显示高密度的区域包括大脑皮层、小脑分子层、边缘系统的部分区域、嗅球、下丘脑以及脊髓三叉神经核和脊髓的胶状质。白质区域的受体水平可忽略不计。这些定位显示了大脑的哪些部分受到苯二氮䓬给药的影响，并有助于我们理解这些药物的众所周知的特性（如抗焦虑和抗惊厥作用）的机制。
