LABELING OF PERIPHERAL-TYPE BENZODIAZEPINE BINDING-SITES IN HUMAN-BRAIN WITH [H-3] PK-11195 - ANATOMICAL AND SUBCELLULAR-DISTRIBUTION
LABELING OF PERIPHERAL-TYPE BENZODIAZEPINE BINDING-SITES IN HUMAN-BRAIN WITH [H-3] PK-11195 - ANATOMICAL AND SUBCELLULAR-DISTRIBUTION
复制标题
DOI：
10.1016/0361-9230(87)90033-5
复制
发表时间：
1987-01-01
影响因子：
3.8
通讯作者：
LEFUR, G
中科院分区：
文献类型：
--
作者：
DOBLE, A;MALGOURIS, C;LEFUR, G
外周型苯二氮卓类结合位点以前在啮齿动物和猫脑中表征，现在已使用[3 H]PK 11195在死后人脑中表征。该配体结合的动力学和药理学性质与其他地方的外周型苯二氮卓类结合位点相似。RO 5 -4864在人脑中对该位点的效力接近于反刍动物和食肉动物组织中观察到的效力，但远低于啮齿动物组织中的效力。这些结合位点的区域分布表明是神经元而不是神经胶质定位。[3 H]PK 11195以类似的方式与人脑的载玻片切片结合，从而可以对外周型苯二氮卓类结合位点的区域分布进行定量研究。结合位点分布不均匀，但仅限于灰质。最高密度的结合位点被发现在前脑结构。定位不限于任何功能系统，也不类似于任何先前描述的发射机系统。外周型苯二氮卓类药物结合位点在人类和猫的大脑中的药理学特征和它们的区域和亚细胞分布方面的相似性表明，猫，而不是大鼠，可能是更好的模型，用于研究该网站在人类大脑功能中可能的作用。
The peripheral-type benzodiazepine binding site, erstwhile characterized in the rodent and feline brain, has now been characterized in post-mortem human brain using [3H]PK 11195. The kinetics and pharmacological properties of the binding of this ligand are simliar to peripheral-type benzodiazepine binding sites elsewhere. The potency of RO5-4864 for this site in human brain is close to that seen in ruminate and carnivore tissues but considerably lower than in rodent tissues. The regional distribution of these binding sites would suggest a neuronal rather than a glial localization. [3H]PK 11195 bound in a similar fashion to slide-mounted sections of human brain, thus allowing quantitative studies of the regional distribution of peripheral-type benzodiazepine binding sites to be made. The binding sites were distributed heterogeneously, but were restricted to the grey matter. Highest densities of binding sites were found in forebrain structures. The localization was not limited to any functional system, nor did it resemble any previously described transmitter system. The similarities between peripheral-type benzodiazepine binding sites in human and in feline brain in terms of their pharmacological characteristics and their regional and subcellular distribution suggest that the cat, rather than the rat, may be the better model for studying a possible role for this site in human cerebral function.