Zlobina G P, Chekalina N D
Zh Nevropatol Psikhiatr Im S S Korsakova. 1987;87(7):1043-5.
Specific binding of 3H-domperidone was detected in a homogenate of human caudate nucleus tissue obtained from mentally healthy people and schizophrenic patients postmortem. Analysis of Scatchard's graph revealed only one type of binding sites with a dissociation constant of about 17 nM and the maximal number of binding sites about 87 pmol/g of the initial tissue. According to the current concepts, 3H-domperidone is a selective ligand of D2 dopamine receptors mediating the psychotropic effect of neuroleptics. The use of human brain for the investigation of these receptors may contribute to the elucidation of the mechanism of action of psychotropic drugs.
在取自心理健康者及精神分裂症患者死后的人脑尾状核组织匀浆中检测到了³H-多潘立酮的特异性结合。对Scatchard图的分析显示只有一种结合位点,其解离常数约为17 nM,结合位点的最大数量约为87 pmol/g初始组织。根据目前的概念,³H-多潘立酮是D2多巴胺受体的选择性配体,介导抗精神病药物的精神otropic作用。用人脑研究这些受体可能有助于阐明精神otropic药物的作用机制。