Zajac J M, Gully D, Maffrand J P
Laboratoire de Pharmacologie et de Toxicologie Fondamentales, CNRS, Toulouse, France.
J Recept Signal Transduct Res. 1996 Jan-Mar;16(1-2):93-113. doi: 10.3109/10799899609039943.
The binding and distribution of radiolabelled SR27897B, a potent CCK-A antagonist, was characterized using in vitro receptor autoradiography. Rapid imaging and quantitative analysis of [3H]SR27897B binding was obtained in a very short period of time (5 days) with a highly sensitive radioimager ensuring very short exposure times for isotopes such as tritium. Tritiated SR27897B binding sites are localized almost exclusively in the area postrema and the medical part of the nucleus tractus solitarius and in this nucleus the rostral-caudal distribution of CCK-A sites differed from that of sulphated CCK8 receptors. Receptor binding properties analyzed on 15 microns serial coronal sections showed on site receptor occupancy in these two regions with high affinity and selectivity characteristic of the CCK-A receptor. These results precisely locate the SR27897B binding sites and provide further support for the absence of heterogeneity of the CCK-A receptors in the rat brain.
使用体外受体放射自显影技术对强效CCK - A拮抗剂放射性标记的SR27897B的结合与分布进行了表征。利用高灵敏度放射性成像仪，在极短时间（5天）内获得了[3H]SR27897B结合的快速成像和定量分析结果，确保了诸如氚等同位素的极短曝光时间。氚标记的SR27897B结合位点几乎仅定位于最后区和孤束核的内侧部分，并且在该核中，CCK - A位点的头 - 尾分布与硫酸化CCK8受体的分布不同。在15微米连续冠状切片上分析的受体结合特性显示，在这两个区域存在具有CCK - A受体高亲和力和选择性特征的位点受体占据情况。这些结果精确地定位了SR27897B结合位点，并为大鼠脑中CCK - A受体不存在异质性提供了进一步支持。
