Gehlert D R, Gackenheimer S L, Wong D T, Robertson D W
Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285.
Brain Res. 1991 Jul 5;553(1):149-54. doi: 10.1016/0006-8993(91)90242-n.
5-HT3 receptors have been localized in the rat brain using the selective antagonist ligand [3H]LY278584. The binding of this ligand to slide mounted tissue sections was characterized by a Kd value of 1.5 nM and a Bmax value of 110 fmol/mg tissue dry weight. The specific binding was displaced by 5-HT or a number of 5-HT3 antagonist compounds. High densities of 5-HT3 receptors were detected in the nucleus of the solitary tract, dorsal motor nucleus of the vagus and area postrema. Moderate levels of binding were found in the glomerular layer of the olfactory bulb, substantia gelatinosa of the trigeminal nucleus and spinal cord and various nuclei of the amygdala. Low levels of binding were found in the superficial laminae of the cerebral cortex and relatively evenly distributed in the hippocampus. These results indicate that [3H]LY278584 is a useful ligand to study 5-HT3 receptors by quantitative autoradiography.
使用选择性拮抗剂配体[3H]LY278584已在大鼠脑中定位了5-羟色胺3（5-HT3）受体。该配体与载玻片上组织切片的结合特征为解离常数（Kd）值为1.5纳摩尔，最大结合容量（Bmax）值为110飞摩尔/毫克组织干重。5-羟色胺（5-HT）或多种5-HT3拮抗剂化合物可取代特异性结合。在孤束核、迷走神经背运动核和最后区检测到高密度的5-HT3受体。在嗅球的肾小球层、三叉神经核的胶状质、脊髓以及杏仁核的各个核中发现中等水平的结合。在大脑皮层的浅层发现低水平的结合，并且在海马体中相对均匀分布。这些结果表明，[3H]LY278584是通过定量放射自显影研究5-HT3受体的有用配体。
