In vivo binding of [3H]ketanserin on serotonin S2-receptors in rat brain.
In vivo binding of [3H]ketanserin on serotonin S2-receptors in rat brain.
复制标题
[3H]酮色林在大鼠脑中血清素 S2 受体上的体内结合。
DOI：
10.1016/0014-2999(82)90599-4
复制
发表时间：
1982
影响因子：
5
通讯作者：
J. Leysen
中科院分区：
文献类型：
--
作者：
P. Laduron;P. Janssen;J. Leysen
本文研究了[~3H]酮丝氨酸在大鼠不同脑区的活体结合。静脉注射后。注射[3 H]酮丝氨酸(5μg·kg−1)后，额叶皮质标记最强。标记药物的脑处置与体外检测到的5-羟色胺S2受体的分布有关。这种结合在5-羟色胺能区是饱和的，但在小脑不是。测试了各种药物取代或阻止[~3H]酮丝氨酸结合的能力；然后将这些结果与在额叶皮质使用[~H]螺环酮的结果进行了比较。虽然[~3H]螺环酮可以用来区分药物对5-羟色胺(额叶皮质)和多巴胺(纹状体)受体的亲和力，但[~3H]酮丝氨酸的最大优势是它只标记5-羟色胺S2受体。
In vivo binding of [3H]ketanserin was studied in various brain regions in rats. After i.v. injection of [3H]ketanserin (5 μg·kg−1), the highest labelling was found in the frontal cortex. Brain disposition of labelled drug correlated with the distribution of serotonin S2-receptors detected in vitro. The binding was saturable in the serotonergic areas but not in the cerebellum. Various drugs were tested for their ability to displace or to prevent [3H]ketanserin binding; these results were then compared to those obtained with [3H]spiperone in the frontal cortex. Although [3H]spiperone can be used to differentiate the affinity of a drug for serotonin (frontal cortex) and dopamine (striatum) receptors, the great advantage of [3H]ketanserin is that it labels serotonin S2-receptors exclusively.