McLean S, Weber E
Laboratory of Neurophysiology, National Institute of Mental Health, Bethesda, MD 20892.
Neuroscience. 1988 Apr;25(1):259-69. doi: 10.1016/0306-4522(88)90024-3.
The distribution of sigma receptors in guinea-pig brain is demonstrated using quantitative autoradiography and the new selective sigma receptor probe, 1,3-di(2[5-(3)H]tolyl)guanidine. Pharmacological analysis, using slide-mounted brain sections, reveals that this site is saturable and has a drug-specificity profile similar to that found in homogenate binding studies. Autoradiography reveals a moderate to high density of discrete, specific labeling superimposed on a lower level of homogeneous 1,3-di(2[5-(3)H]tolyl)guanidine binding. Both patterns are displaced by incubation with 10 microM haloperidol or 1,3-di-ortho-tolyl-guanidine. In the forebrain, the highest density of binding is associated with the magnocellular-neuroendocrine and limbic systems; lower densities are distributed in non-limbic nuclei and the lowest levels occur in the extrapyramidal system. In the midbrain and hindbrain, motor nuclei involved in voluntary and involuntary motor behavior are discretely labeled, as are many of the cranial nerve nuclei. The anatomical distribution of the haloperidol-sensitive sigma receptors is distinct from the pattern of phencyclidine receptors and suggests sigma compounds may effect endocrine, emotional and motor behavior.
利用定量放射自显影技术和新型选择性σ受体探针1,3-二(2-[5-(3)H]甲苯基)胍，展示了豚鼠脑中σ受体的分布。使用载玻片固定的脑切片进行药理学分析表明，该位点具有饱和性，且其药物特异性谱与匀浆结合研究中发现的相似。放射自显影显示，在较低水平的均匀1,3-二(2-[5-(3)H]甲苯基)胍结合之上，叠加有中度到高密度的离散特异性标记。这两种模式均可被10微摩尔氟哌啶醇或1,3-二邻甲苯基胍孵育所取代。在前脑，最高密度的结合与大细胞神经内分泌系统和边缘系统相关；较低密度分布于非边缘核，而最低水平出现在锥体外系。在中脑和后脑，参与自主和非自主运动行为的运动核被离散标记，许多脑神经核也是如此。氟哌啶醇敏感的σ受体的解剖分布与苯环己哌啶受体的模式不同，提示σ化合物可能影响内分泌、情绪和运动行为。
