Waeber C, Dietl M M, Hoyer D, Probst A, Palacios J M
Preclinical Research, Sandoz Ltd., Basel, Switzerland.
Neurosci Lett. 1988 May 16;88(1):11-6. doi: 10.1016/0304-3940(88)90307-2.
The localization of a novel serotonin (5-hydroxytryptamine, 5-HT) recognition site named 5-HT1D was studied by autoradiography in human postmortem brain material. Serotonin-1 sites were labeled with [3H]5-HT. The different subpopulations of 5-HT1 sites were investigated by the use of unlabeled selective compounds. 8-OH-DPAT (8-hydroxy-2-[N,N-di-n-propyl-amino]tetralin) was used to block [3H]5-HT binding to 5-HT1A, the beta-blocker (-)-21 009 (4-[3-ter-butyl-amino-2-hydroxy-propoxy]indol-2-carbonic acid isopropyl ester) to 5-HT1B and the ergoline mesulergine to 5-HT1C recognition sites. 5-HT1D sites were defined as the binding sites remaining when both 8-OH-DPAT and mesulergine were added to the incubation medium. Under these conditions, 5-HT1D sites represented a high proportion of total [3H]5-HT binding sites in the basal ganglia and substantia nigra. Lower proportions were observed in other brain areas such as the hippocampal formation and raphé nuclei. 5-HT1D sites thus represent the majority of 5-HT1 binding sites in the striatonigral pathway in man. This localization suggests an involvement of these sites in the mediation of serotoninergic mechanisms in basal ganglia functions and a possible role in brain diseases where these areas are known to be involved.
通过放射自显影术在人类尸检脑材料中研究了一种名为5-HT1D的新型血清素（5-羟色胺，5-HT）识别位点的定位。用[3H]5-HT标记血清素-1位点。使用未标记的选择性化合物研究了5-HT1位点的不同亚群。8-OH-DPAT（8-羟基-2-[N，N-二正丙基-氨基]四氢萘）用于阻断[3H]5-HT与5-HT1A的结合，β-阻滞剂（-）-21 009（4-[3-叔丁基-氨基-2-羟基-丙氧基]吲哚-2-碳酸异丙酯）用于阻断[3H]5-HT与5-HT1B的结合，麦角灵用于阻断[3H]5-HT与5-HT1C识别位点的结合。5-HT1D位点定义为将8-OH-DPAT和麦角灵都添加到孵育培养基中时剩余的结合位点。在这些条件下，5-HT1D位点在基底神经节和黑质中占总[3H]5-HT结合位点的很大比例。在其他脑区，如海马结构和中缝核中观察到的比例较低。因此，5-HT1D位点代表了人类纹状体黑质通路中5-HT1结合位点的大部分。这种定位表明这些位点参与了基底神经节功能中血清素能机制的介导，并且在已知这些区域受累的脑部疾病中可能发挥作用。
