Benavides J, Guilloux F, Rufat P, Uzan A, Renault C, Dubroeucq M C, Gueremy C, Le Fur G
Eur J Pharmacol. 1984 Mar 16;99(1):1-7. doi: 10.1016/0014-2999(84)90425-4.
'Peripheral type' benzodiazepine binding sites in several rat tissues were labelled by intravenous injection of [3H]PK 11195 and [3H] RO5 -4864. Binding was saturable in all tissues studied and regional distribution paralleled the in vitro binding. A similar potency order of displacing compounds was found in vivo and in vitro PK 11195 greater than PK 11211 greater than RO5 -4864 greater than diazepam greater than dipyridamole greater than clonazepam. These results demonstrate the feasibility of using this technique to examine the effects of pharmacological manipulation on the binding sites in their native state. However some properties (broader maximum during time course, higher percentage of particulate binding in the brain and independence of temperature) make [3H]PK 11195 the most suitable ligand for this kind of studies.
通过静脉注射[3H]PK 11195和[3H]RO5 - 4864对几只大鼠组织中的“外周型”苯二氮䓬结合位点进行标记。在所研究的所有组织中，结合是可饱和的，并且区域分布与体外结合情况相似。在体内和体外发现了类似的取代化合物效力顺序：PK 11195＞PK 11211＞RO5 - 4864＞地西泮＞双嘧达莫＞氯硝西泮。这些结果证明了使用该技术研究药理操作对天然状态下结合位点影响的可行性。然而，一些特性（时间进程中更宽的最大值、脑中颗粒结合的更高百分比以及温度独立性）使得[3H]PK 11195成为这类研究最合适的配体。
