Hall H, Farde L, Halldin C, Hurd Y L, Pauli S, Sedvall G
Karolinska Institutet, Department of Clinical Neuroscience, Karolinska Hospital, Stockholm, Sweden.
Synapse. 1996 Jun;23(2):115-23. doi: 10.1002/(SICI)1098-2396(199606)23:2<115::AID-SYN7>3.0.CO;2-C.
Epidepride is a benzamide with high affinity for central D2- and D3-dopamine receptors. The anatomical distribution of [125I]epidepride binding was examined by autoradiography, using postmortem human whole-hemisphere cryosections. The density of [125I]epidepride binding sites was high in caudate nucleus and putamen. [125I]epidepride also labeled receptors in extrastriatal region such as in the pallidum, some thalamic nuclei, the neocortex, and the substantia nigra. The neocortical binding was heterogeneously distributed. In most cortical regions, binding sites were located in superficial layers (I-II). However, in basal levels of the occipital cortex, [125I]epidepride binding was located in a deeper layer, probably corresponding to layer V. Competition studies indicated that most of the [125I]epidepride binding represented predominantly D2-dopamine receptors, in striatal as well as in extrastriatal regions. The presence of extrastriatal D2-dopamine receptor populations is of particular interest for research on schizophrenia and antipsychotic drug action.
表哌立登是一种对中枢D2和D3多巴胺受体具有高亲和力的苯甲酰胺。使用死后人类全脑半球冷冻切片，通过放射自显影检查了[125I]表哌立登结合的解剖分布。[125I]表哌立登结合位点在尾状核和壳核中的密度很高。[125I]表哌立登还标记了纹状体以外区域的受体，如苍白球、一些丘脑核、新皮层和黑质。新皮层结合呈异质性分布。在大多数皮质区域，结合位点位于表层（I-II层）。然而，在枕叶皮质的基底部，[125I]表哌立登结合位于更深的层，可能对应于V层。竞争研究表明，在纹状体以及纹状体以外区域，大多数[125I]表哌立登结合主要代表D2多巴胺受体。纹状体以外D2多巴胺受体群体的存在对于精神分裂症和抗精神病药物作用的研究尤为重要。
