Voigt M M, Laurie D J, Seeburg P H, Bach A
Laboratory of Molecular Neuroendocrinology, University of Heidelberg, FRG.
EMBO J. 1991 Dec;10(13):4017-23. doi: 10.1002/j.1460-2075.1991.tb04977.x.
To date, there have been at least eight different receptors for the neurotransmitter serotonin (5-HT) identified in the central nervous system. These receptors fall into four pharmacological classes: 5-HT1, 5-HT2, 5-HT3 and 5-HT4. The 5-HT1 class has been shown to contain at least four pharmacologically distinct subtypes, 5-HT1A-D. Of these, cDNAs encoding the 5-HT1A and 5-HT1C receptors have been previously characterized. We now report the cloning and expression of a rat brain cDNA encoding another member of the 5-HT1 receptor family. Transient expression of this clone demonstrated high-affinity binding of [3H]5-HT with a pharmacological profile corresponding to that of the 5-HT1B subtype: 5-CT, 5-HT greater than propranolol greater than methysergide greater than rauwolscine greater than 8-OH-DPAT. In situ hybridization revealed expression of cognate mRNA within cells of the dorsal and median raphe nuclei, consistent with previous reports that the 5-HT1B receptor acts as an autoreceptor on 5-HT terminals in this species. mRNA expression was also detected in cells within the CA1 region of hippocampus, striatum, layer 4 of cortex and in the cerebellum, suggesting a previously unrecognized post-synaptic role for the 5-HT1B receptor.
迄今为止，在中枢神经系统中已鉴定出至少八种不同的神经递质5-羟色胺（5-HT）受体。这些受体分为四个药理学类别：5-HT1、5-HT2、5-HT3和5-HT4。已证明5-HT1类别包含至少四种药理学上不同的亚型，即5-HT1A-D。其中，编码5-HT1A和5-HT1C受体的cDNA先前已得到表征。我们现在报告编码5-HT1受体家族另一个成员的大鼠脑cDNA的克隆和表达。该克隆的瞬时表达显示[3H]5-HT具有高亲和力结合，其药理学特征与5-HT1B亚型相对应：5-CT、5-HT大于普萘洛尔大于甲基麦角新碱大于萝芙木碱大于8-OH-DPAT。原位杂交显示在背侧和中缝核的细胞内有同源mRNA表达，这与先前关于5-HT1B受体在该物种中作为5-HT终末上的自身受体起作用的报道一致。在海马CA1区、纹状体、皮质第4层以及小脑中的细胞内也检测到了mRNA表达，这表明5-HT1B受体具有先前未被认识到的突触后作用。
