Bischoff S, Bittiger H, Krauss J
Eur J Pharmacol. 1980 Dec 5;68(3):305-15. doi: 10.1016/0014-2999(80)90528-2.
The existence of DA receptors in the rat hippocampus was demonstrated with an in vivo [3H]spiperone radioreceptor assay. Kinetic studies revealed that maximum binding of [3H]spiperone in hippocampus was much smaller than in striatum and frontal cortex but much higher than in cerebellum. In inhibition studies of [3H]spiperone binding, all neuroleptics tested were active in hippocampus as well as in striatum. In contrast, 5HT antagonists were definitely less potent in these two brain regions than in frontal cortex. Finally, even when 5HT receptors were blocked, dipropyl-ATN and haloperidol remained fully effective in hippocampus, striatum, but also in frontal cortex although to a lesser degree. From these results it was concluded that [3H]spiperone binds mainly to DA receptors in hippocampus as well as in striatum, whereas both 5HT and DA receptors are present in frontal cortex.
采用体内[3H]螺哌隆放射性受体分析法证实了大鼠海马中存在多巴胺(DA)受体。动力学研究表明,[3H]螺哌隆在海马中的最大结合量远小于纹状体和额叶皮质,但远高于小脑。在[3H]螺哌隆结合抑制研究中,所有测试的抗精神病药物在海马和纹状体中均有活性。相比之下,5-羟色胺(5HT)拮抗剂在这两个脑区的效力肯定低于额叶皮质。最后,即使5HT受体被阻断,二丙基-ATN和氟哌啶醇在海马、纹状体以及额叶皮质中仍保持完全有效,尽管在额叶皮质中的效果稍弱。从这些结果可以得出结论,[3H]螺哌隆主要与海马和纹状体中的DA受体结合,而额叶皮质中同时存在5HT和DA受体。