In vivo activity of the thyroid hormone receptor β- and α-selective agonists GC-24 and CO23 on rat liver, heart, and brain

Carmen Grijota-Martínez, Eric Samarut, Thomas S. Scanlan, Beatriz Morte, Juan Bernal

Research output: Contribution to journalArticle

24 Scopus citations

Abstract

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,westudied the in vivo activity in developing rats of two thyroid hormone agonists, the TRβ-selective GC-24 and the TRβ-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 TRβ and lacked activity on the brain. On the other hand, CO23 was active in liver, heart, and brain on genes regulated by either TRα or TRβ. This compound, previously shown to be TRα-selective in tadpoles, displayed no selectivity in the rat in vivo.

Original languageEnglish (US)
Pages (from-to)1136-1142
Number of pages7
JournalEndocrinology
Volume152
Issue number3
DOIs
StatePublished - Mar 2011

ASJC Scopus subject areas

  • Endocrinology

Fingerprint Dive into the research topics of 'In vivo activity of the thyroid hormone receptor β- and α-selective agonists GC-24 and CO23 on rat liver, heart, and brain'. Together they form a unique fingerprint.

  • Cite this