Ieni J R, Zukin S R, Van Praag H M
Eur J Pharmacol. 1984 Nov 27;106(3):669-72. doi: 10.1016/0014-2999(84)90078-5.
Scatchard analysis of [3H]imipramine binding to human platelets over the concentration range of 0.1-250 nM revealed a biphasic concave upward curve. Computer-assisted analysis indicated the best fit of the data by a two-site model with apparent Kd values of 0.68 and 293 nM and apparent Bmax values of 802 fmol/mg protein and 12.72 pmol/mg protein for the high- and low-affinity components, respectively. These results demonstrate the complex manner in which [3H]imipramine binding to human platelets, suggesting a reason for inconsistencies in Bmax values reported in the literature. Further studies of these low- as well as high-affinity sites may help elucidate the functional role of [3H]imipramine binding sites in affective disorders.
对[³H]丙咪嗪在0.1 - 250 nM浓度范围内与人血小板结合进行的Scatchard分析显示出一条向上凹的双相曲线。计算机辅助分析表明,数据最适合用双位点模型,高亲和力组分和低亲和力组分的表观解离常数(Kd)值分别为0.68和293 nM,表观最大结合容量(Bmax)值分别为802 fmol/mg蛋白质和12.72 pmol/mg蛋白质。这些结果证明了[³H]丙咪嗪与人血小板结合的复杂方式,这也解释了文献中报道的最大结合容量值不一致的原因。对这些低亲和力和高亲和力位点的进一步研究可能有助于阐明[³H]丙咪嗪结合位点在情感障碍中的功能作用。