RT Journal Article
T1 In Vivo Activity of the Thyroid Hormone Receptor β- and α-Selective Agonists GC-24 and CO23 on Rat Liver, Heart, and Brain
A1 Grijota Martínez, María Carmen
A1 Samarut, Eric
A1 Scanlan, Thomas
A1 Morte, Beatriz
A1 Bernal, Juan
AB 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 TRβ-selective GC-24 and the TRα-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.
PB Oxford University Press
SN 0013-7227
YR 2011
FD 2011
LK https://hdl.handle.net/20.500.14352/92113
UL https://hdl.handle.net/20.500.14352/92113
LA eng
NO Grijota-Martínez, Carmen, et al. «In Vivo Activity of the Thyroid Hormone Receptor β- and α-Selective Agonists GC-24 and CO23 on Rat Liver, Heart, and Brain». Endocrinology, vol. 152, n.o 3, marzo de 2011, pp. 1136-42. DOI.org (Crossref), https://doi.org/10.1210/en.2010-0813.
NO Ministerio de Ciencia e Innovación (España)
NO European Commission
NO Centro de Investigación Biomédica en Enfermedades Raras (España)
NO Instituto de Salud Carlos III
NO National Institutes of Health 
DS Docta Complutense
RD 10 abr 2025