Segu L, Chauveau J, Boulenguez P, Morel A, Lanoir J, Delaage M
C.N.R.S. Laboratoire de Neurobiologie, Marseille.
C R Acad Sci III. 1991;312(13):655-61.
We describe here the synthesis of a new serotonin conjugate, S-CM-GTNH2, and its radioiodinated derivative. Quantitative autoradiographic studies on rat and guinea pig brain sections incubated with 2 nM [3H]5-HT showed a preferential affinity of S-CM-GTNH2 for 5-HT1B and 5-HT1D sites. Autoradiograms from brain sections incubated with 0.02 nM S-CM-G[125I]TNH2 showed a heterogeneous anatomical distribution of the labelling with high densities in regions rich in 5-HT1B or 5-HT1D binding sites, and with no labelling of those rich in 5-HT1A or 5-HT1C sites. The pharmacological profiles of the binding sites corresponded to those of 5-HT1B and 5-HT1D receptor subtypes. The radioligand S-CM-G[125I]TNH2 is a good probe for the study of these sites and will be used for their subcellular localization in electron microscopy.
我们在此描述了一种新型血清素缀合物S-CM-GTNH2及其放射性碘化衍生物的合成。对用2 nM [3H]5-HT孵育的大鼠和豚鼠脑切片进行的定量放射自显影研究表明，S-CM-GTNH2对5-HT1B和5-HT1D位点具有优先亲和力。用0.02 nM S-CM-G[125I]TNH2孵育的脑切片放射自显影片显示，标记的解剖分布不均一，在富含5-HT1B或5-HT1D结合位点的区域密度高，而在富含5-HT1A或5-HT1C位点的区域无标记。结合位点的药理学特征与5-HT1B和5-HT1D受体亚型的特征相符。放射性配体S-CM-G[125I]TNH2是研究这些位点的良好探针，将用于电子显微镜下它们的亚细胞定位。
