Kazawa T, Mikuni M, Higuchi T, Arai I, Takahashi K, Yamauchi T
Department of Psychiatry, Saitama Medical School, Japan.
Life Sci. 1990;47(6):531-7. doi: 10.1016/0024-3205(90)90613-v.
We investigated the pharmacological properties of the sulpiride-displaceable binding sites labeled by 3H-YM-09151-2 in rat frontal cortex, compared to those in striatum. The IC50 value of ketanserin was 486 nM, which was apparently different from its affinity for the 5HT-2 receptor. Various dopamine antagonists showed almost the same inhibitory effects for binding site in frontal cortex and striatum. Sulpiride-displaceable 3H-YM-09151-2 binding sites were considered to be D-2 dopamine receptors. After subchronic treatment with haloperidol, the D-2 receptor density of frontal cortex (0.55 fmol/mg tissue) increased to the same extent (about 25%) as striatum without significant change in apparent affinity.
我们研究了与纹状体相比，大鼠额叶皮质中由3H-YM-09151-2标记的舒必利可置换结合位点的药理学特性。酮色林的IC50值为486 nM，这与其对5HT-2受体的亲和力明显不同。各种多巴胺拮抗剂对额叶皮质和纹状体中的结合位点显示出几乎相同的抑制作用。舒必利可置换的3H-YM-09151-2结合位点被认为是D-2多巴胺受体。用氟哌啶醇进行亚慢性治疗后，额叶皮质的D-2受体密度（0.55 fmol/mg组织）与纹状体以相同程度（约25%）增加，表观亲和力无显著变化。
