Bénavidès J, Savaki H E, Malgouris C, Laplace C, Daniel M, Begassat F, Desban M, Uzan A, Dubroeucq M C, Renault C
Brain Res Bull. 1984 Jul;13(1):69-77. doi: 10.1016/0361-9230(84)90009-1.
"Peripheral type" benzodiazepine binding sites were labelled in cat brain membranes by using [3H]PK 11195. This ligand binds to the "peripheral type" binding sites in a reversible, specific and saturable manner. Cat brain binding sites density (congruent to 6 pmol/mg prot.) was higher than in the rat. Pharmacological specificity was demonstrated by the potency order of displacing agents: PK 11195 greater than RO5-4864 greater than dipyridamole greater than diazepam greater than clonazepam. A similar characterization was performed in slide mounted brain sections where [3H]PK 11195 also labelled the "peripheral type" benzodiazepine binding sites. The high percentage of specific binding (80%) at 1 nM of [3H]PK 11195 made possible the autoradiographic studies on binding sites distribution. These sites were heterogeneously distributed in the grey matter and absent in white matter. Visual, auditory and other specific sensory relay stations were highly labelled. The blood pressure regulating nuclei, the vestibulo-cerebellar and the extrapyramidal motor system also presented a very high binding density. As previously described in the rat brain, choroid plexus was also strongly labelled by [3H]PK 11195 in the cat.
通过使用[3H]PK 11195对猫脑膜中的“外周型”苯二氮䓬结合位点进行标记。该配体以可逆、特异性和饱和的方式与“外周型”结合位点结合。猫脑结合位点密度（约6 pmol/mg蛋白）高于大鼠。通过置换剂的效力顺序证明了药理学特异性：PK 11195＞RO5 - 4864＞双嘧达莫＞地西泮＞氯硝西泮。在载玻片上的脑切片中进行了类似的表征，其中[3H]PK 11195也标记了“外周型”苯二氮䓬结合位点。1 nM的[3H]PK 11195时高比例的特异性结合（80%）使得对结合位点分布进行放射自显影研究成为可能。这些位点在灰质中分布不均，在白质中不存在。视觉、听觉和其他特定感觉中继站标记明显。血压调节核、前庭小脑和锥体外系运动系统也呈现出非常高的结合密度。如先前在大鼠脑中所描述的，脉络丛在猫中也被[3H]PK 11195强烈标记。
