Reynolds G P, Mason S L
Department of Biomedical Science, University of Sheffield, England, U.K.
J Neurochem. 1994 Oct;63(4):1576-7. doi: 10.1046/j.1471-4159.1994.63041576.x.
The density of dopamine D2-like receptors was determined using [3H]emonapride binding in putamen tissue taken postmortem from schizophrenic subjects and matched controls. A 72% increase in number of these receptors was identified in the schizophrenics, although three patients not receiving antipsychotic drug treatment before death exhibited receptor densities in the control range. Displacement of 1 nM [3H]emonapride binding by raclopride was used to define the contribution of the D4 subtype of dopamine receptors to total [3H]emonapride binding. No evidence was obtained for the presence of D4 receptors in putamen tissue from either control or schizophrenic subjects, indicating that the increase in D2-like receptor density in schizophrenia is due not to an increase in number of D4 sites in the disease, but to an up-regulation of D2 or D3 receptors probably induced by chronic treatment with antipsychotic drugs.
使用[3H]依莫必利结合法测定了精神分裂症患者及匹配对照死后壳核组织中多巴胺D2样受体的密度。在精神分裂症患者中，这些受体数量增加了72%，不过有三名在死亡前未接受抗精神病药物治疗的患者，其受体密度处于对照范围内。用雷氯必利取代1 nM [3H]依莫必利结合，以确定多巴胺受体D4亚型对总[3H]依莫必利结合的贡献。在对照或精神分裂症患者的壳核组织中均未获得存在D4受体的证据，这表明精神分裂症中D2样受体密度的增加并非由于疾病中D4位点数量的增加，而是可能由抗精神病药物的长期治疗诱导的D2或D3受体上调所致。
