INVIVO LABELING IN SEVERAL RAT-TISSUES OF PERIPHERAL TYPE BENZODIAZEPINE BINDING-SITES
INVIVO LABELING IN SEVERAL RAT-TISSUES OF PERIPHERAL TYPE BENZODIAZEPINE BINDING-SITES
复制标题
DOI：
10.1016/0014-2999(84)90425-4
复制
发表时间：
1984-01-01
影响因子：
5
通讯作者：
LEFUR, G
中科院分区：
文献类型：
--
作者：
BENAVIDES, J;GUILLOUX, F;LEFUR, G
通过静脉注射[3 H]PK 11195 [1-（2-氯苯基）-N-甲基-N-（1-甲基丙基）-3-异喹啉甲酰胺]和[3 H] RO 5 -4864 8（7-氯-5-（4-氯苯基）-1，3-二氢-1-甲基-2H-1，4-苯并二氮杂卓-2-酮]标记几种大鼠组织中的外周型苯并二氮杂卓结合位点。结合是饱和的，在所有组织研究和区域分布的体外结合。在体内和体外发现置换化合物的类似效力顺序为PK 11195 > PK 11211 > RO 5 -4864 >地西泮>双嘧达莫>氯硝西泮。这些结果证明了使用这种技术来检查药理学操作对天然状态下结合位点的影响的可行性。某些性质（时间过程中最大值更宽、大脑中颗粒结合百分比更高以及不依赖于温度）使[3 H]PK 11195成为此类研究的最合适配体。
Peripheral type benzodiazepine binding sites in several rat tissues were labeled by i.v. injection of [3H]PK 11195 [1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide] and [3H]RO5-4864 8(7-chloro-5-(4-chlorophenyl)-1,3-dihydro-1-methyl-2H-1,4-benzodiazepin-2-one]. 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 > PK 11211 > RO5-4864 > diazepam > dipyridamole > 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. 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.