Le Fur G, Perrier M L, Vaucher N, Imbault F, Flamier A, Benavides J, Uzan A, Renault C, Dubroeucq M C, Guérémy C
Life Sci. 1983 Apr 18;32(16):1839-47. doi: 10.1016/0024-3205(83)90062-0.
[3H] RO5-4864 binding sites have been characterized in kidney, heart, brain, adrenals and platelets in the rat. In all these organs the following order of potency in the RO5-4864 displacement was found: RO5-4864 greater than diazepam greater than clonazepam indicating that they correspond to the "peripheral type" of benzodiazepine binding sites. PK 11195, an isoquinoline carboxamide derivative, displaces [3H] RO5-4864 from its binding sites in all the organs. PK 11195 was as potent as RO5-4864 in the platelets, heart, adrenals, kidney and several brain regions (midbrain, hypothalamus, medulla + pons and hippocampus. However it was 5 to 10 times more effective in cortex and striatum. In conclusion PK 11195 might represent a new tool to elucidate the physiological relevance of "peripheral type" benzodiazepine binding sites and might help to discriminate the hypothetical subclasses of these binding sites.
已对大鼠的肾脏、心脏、大脑、肾上腺和血小板中的[3H] RO5 - 4864结合位点进行了表征。在所有这些器官中，发现RO5 - 4864取代的效力顺序如下：RO5 - 4864大于地西泮大于氯硝西泮，这表明它们对应于苯二氮䓬结合位点的“外周型”。PK 11195是一种异喹啉甲酰胺衍生物，可在所有器官中从其结合位点取代[3H] RO5 - 4864。PK 11195在血小板、心脏、肾上腺、肾脏和几个脑区（中脑、下丘脑、延髓+脑桥和海马体）中的效力与RO5 - 4864相当。然而，它在皮质和纹状体中的效力要高5至10倍。总之，PK 11195可能是一种新工具，用于阐明“外周型”苯二氮䓬结合位点的生理相关性，并可能有助于区分这些结合位点的假设亚类。
