Choi D S, Colas J F, Kellermann O, Loric S, Launay J M, Rosay P, Maroteaux L
Laboratoire de Génétique Moléculaire des Eucaryotes du CNRS, U184 de Génétique, et de Biologie Moléculaire de l'INSERM, Faculté de Médecine de Strasbourg, France.
Cell Mol Biol (Noisy-le-grand). 1994 May;40(3):403-11.
The novel serotonin receptor 5-HT2B shows the highest homology to the 5-HT2 family of receptors. The pharmacological profile of membranes from 5-HT2B cDNA stably transfected LMTK- cell line, corresponds to a new 5-HT2-like receptor named 5-HT2B, although some difference exists between the mouse and rat pharmacology. A similar pharmacological profile is detected on the immortalized teratocarcinoma-derived cell line 1C11 upon 2 days of serotoninergic differenciation by cAMP. In both cell lines, the analysis 125I-DOI binding reveals the presence of a single class of sites, the affinity of which is one order of magnitude lower than the one reported for the 5-HT2A receptor. This demonstrates that the 5-HT2B receptor is functionally expressed before the complete serotoninergic differentiation of 1C11 cells. These observations are in good agreement with the presence of 5-HT2B mRNA in early mouse embryonic development. Furthermore, the major sites of 5-HT2B mRNA embryonic expression are in the heart, and in the neural fold before the closure of the neural tube. Therefore, this receptor could account at least in part for the trophic functions attributed to the 5-HT2-like receptors.
新型5-羟色胺受体5-HT2B与5-HT2受体家族具有最高的同源性。来自稳定转染5-HT2B cDNA的LMTK-细胞系的膜的药理学特征,与一种名为5-HT2B的新型5-HT2样受体相对应,尽管小鼠和大鼠的药理学之间存在一些差异。在通过cAMP进行5-羟色胺能分化2天后,在永生化的畸胎瘤衍生细胞系1C11上检测到类似的药理学特征。在这两种细胞系中,125I-DOI结合分析显示存在单一类别的位点,其亲和力比报道的5-HT2A受体低一个数量级。这表明5-HT2B受体在1C11细胞完全5-羟色胺能分化之前就已功能性表达。这些观察结果与5-HT2B mRNA在小鼠早期胚胎发育中的存在情况高度一致。此外,5-HT2B mRNA胚胎表达的主要部位在心脏以及神经管闭合前的神经褶中。因此,该受体至少可以部分解释归因于5-HT2样受体的营养功能。