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首页> 外文期刊>Endocrinology >In vivo activity of the thyroid hormone receptor beta- and alpha-selective agonists GC-24 and CO23 on rat liver, heart, and brain.
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In vivo activity of the thyroid hormone receptor beta- and alpha-selective agonists GC-24 and CO23 on rat liver, heart, and brain.

机译：甲状腺激素受体β-和α-选择性激动剂GC-24和CO23对大鼠肝脏，心脏和大脑的体内活性。

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摘要

Thyroid hormone analogs with selective actions through specific thyroid hormone receptor (TR) subtypes are of great interest. They might offer the possibility of mimicking physiological actions of thyroid hormone with receptor subtype or tissue specificity with therapeutic aims. They are also pharmacological tools to dissect biochemical pathways mediated by specific receptor subtypes, in a complementary way to mouse genetic modifications. In this work, we studied the in vivo activity in developing rats of two thyroid hormone agonists, the TRbeta-selective GC-24 and the TRalpha-selective CO23. Our principal goal was to check whether these compounds were active in the rat brain. Analog activity was assessed by measuring the expression of thyroid hormone target genes in liver, heart, and brain, after administration to hypothyroid rats. GC-24 was very selective for TRbeta and lacked activity on the brain. On the other hand, CO23 was active in liver, heart, and brain on genes regulated by either TRalpha or TRbeta. This compound, previously shown to be TRalpha-selective in tadpoles, displayed no selectivity in the rat in vivo.
机译：通过特定的甲状腺激素受体（TR）亚型具有选择性作用的甲状腺激素类似物引起了极大的兴趣。他们可能提供模仿具有治疗目的的受体亚型或组织特异性的甲状腺激素的生理作用的可能性。它们还是以与小鼠基因修饰互补的方式剖析由特定受体亚型介导的生化途径的药理学工具。在这项工作中，我们研究了两种甲状腺激素激动剂TRbeta选择性GC-24和TRalpha选择性CO23在发育中的大鼠的体内活性。我们的主要目标是检查这些化合物在大鼠脑中是否具有活性。在对甲状腺功能减退的大鼠给药后，通过测量肝脏，心脏和大脑中甲状腺激素靶基因的表达来评估类似物的活性。 GC-24对TRbeta非常有选择性，并且对大脑缺乏活性。另一方面，CO23在肝，心和脑中对受TRalpha或TRbeta调控的基因有活性。先前在t中显示出对TRalpha选择性的这种化合物在大鼠体内没有显示出选择性。

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