Waeber C, Hoyer D, Palacios J M
Preclinical Research, Sandoz Ltd, Basle, Switzerland.
Neuroscience. 1989;31(2):393-400. doi: 10.1016/0306-4522(89)90382-5.
The distribution of 5-hydroxytryptamine receptors of the 5-hydroxytryptamine3 type was examined in human brain post mortem tissue, using quantitative in vitro autoradiography. The selective and potent 5-hydroxytryptamine3 receptor antagonist [3H]ICS 205-930 [(3 alpha-tropanyl)-1H-indole-3-carboxylic acid ester] was used as ligand. Highest levels of labelling were found in discrete nuclei of the lower brainstem. At all levels of the spinal cord the substantia gelatinosa was also densely labelled. In contrast, specific binding in the forebrain was very low and concentrated in some regions of the limbic system. The enrichment of [3H]ICS 205-930 binding sites in nuclei of the dorsal medulla and spinal cord is in good agreement with the proposed role for 5-hydroxytryptamine in sensory processing. High densities of 5-hydroxytryptamine3 binding sites in the area postrema support a central site of action for 5-hydroxytryptamine in emesis. Finally, the presence of [3H]ICS 205-930 binding sites in the limbic system provides an anatomical substrate for the behavioural effects of 5-hydroxytryptamine3 receptor antagonists.
利用定量体外放射自显影技术，对人死后脑组织中5-羟色胺3型5-羟色胺受体的分布进行了研究。选择性强效5-羟色胺3受体拮抗剂[3H]ICS 205-930[（3α-托烷基）-1H-吲哚-3-羧酸酯]用作配体。在脑干下部的离散核中发现了最高水平的标记。在脊髓的所有层面，胶状质也有密集标记。相比之下，前脑中的特异性结合非常低，且集中在边缘系统的一些区域。[3H]ICS 205-930结合位点在延髓背侧核和脊髓中的富集与5-羟色胺在感觉处理中的作用相符。最后，5-羟色胺3结合位点在最后区的高密度分布支持了5-羟色胺在呕吐中的中枢作用位点。最后，边缘系统中[3H]ICS 205-930结合位点的存在为5-羟色胺3受体拮抗剂的行为效应提供了解剖学基础。
