Burman K D, Lukes Y G, Latham K R, Wartofsky L
Horm Metab Res. 1980 Dec;12(12):685-7. doi: 10.1055/s-2007-999232.
We have determined that 8-anilino-1-naphthalene sulfonic acid (ANS) and ipodate are effective inhibitor in vitro of 125I-T3 binding to rat hepatic nuclei receptors. Both of these agents are estimated to have a Kd for the T3 receptor of about 1--2 x 10(-4) M. Indirect preliminary studies suggest that ANS is a non-competitive inhibitor and ipodate is a competitive inhibitor of T3 binding. Compounds such as tyropanoate and diatrizoate and iodide had no effect on T3 receptor binding. Further in vivo studies with ipodate suggested that T3 receptor binding inhibition also occurred when ipodate was given intravenously to rats.
我们已经确定,8-苯胺基-1-萘磺酸(ANS)和碘番酸在体外是125I-T3与大鼠肝细胞核受体结合的有效抑制剂。据估计,这两种药物对T3受体的解离常数(Kd)约为1-2×10^(-4)M。间接初步研究表明,ANS是一种非竞争性抑制剂,碘番酸是T3结合的竞争性抑制剂。诸如酪氨酸泛影酸盐、泛影酸盐和碘化物等化合物对T3受体结合没有影响。对碘番酸进行的进一步体内研究表明,当给大鼠静脉注射碘番酸时,也会发生T3受体结合抑制。