Effect of thyroid hormone analogues on the displacement of 125I-L-triiodothyronine from hepatic and heart nuclei in vivo: possible relationship to hormonal activity.
Effect of thyroid hormone analogues on the displacement of 125I-L-triiodothyronine from hepatic and heart nuclei in vivo: possible relationship to hormonal activity.
复制标题
甲状腺激素类似物对体内肝和心核中 125I-L-三碘甲状腺原氨酸置换的影响：与激素活性的可能关系。
DOI：
10.1016/0006-291x(73)91177-7
复制
发表时间：
1973
影响因子：
3.1
通讯作者：
M. I. Surks
中科院分区：
文献类型：
--
作者：
J. H. Oppenheimer;Harold L. Schwartz;W. Dillman;M. I. Surks
碘酪氨酸和碘甲状腺原氨酸类似物从大鼠肝和心脏特异性核结合位点置换示踪剂[125 I] L-3，5，3 ′-三碘甲状腺原氨酸的能力与非放射性三碘甲状腺原氨酸的置换能力有关。碘酪氨酸和L-3，3 ′，5 ′三碘甲状腺原氨酸（“反向T3”）没有置换活性。在酚环的“内环”上有3，5取代，而在3′位上有一个“本体”取代的类似物表现出最强的置换活性。当考虑到类似物的分布、分数去除率和代谢转化时，置换活性似乎与报告的拟甲状腺活性相关。这些结果支持了核场址的生物相关性。
The capacity of iodotyrosines and iodothyronine analogues to displace tracer[125I] L-3,5,3′ triiodothyronine from specific nuclear binding sites in rat liver and heart was related to the displacement capacity of nonradioactive triiodothyronine. Iodotyrosines and L-3,3′,5′ triiodothyronine (“reverse T3”) were devoid of displacement activity. Analogues with 3,5 substitution in the “inner” ring and single “bulk” substitution in the 3′ position in the phenolic ring exhibited the strongest displacement activity. When the distribution, fractional removal rates and metabolic conversion of the analogues were taken into account, displacement activity appeared to correlate well with the reported thyromimetic activity. These results support the biologic relevance of the nuclear sites.