Thyroid hormone receptor β-specific agonist GC-1 increases energy expenditure and prevents fat-mass accumulation in rats
Open accessAbstract
It is well known that thyroid hormone affects body composition; however, the effect of the thyroid hormone receptor β (TRβ)-selective thyromimetic GC-1 on this biological feature had not been demonstrated. In the current study, we compared the effects of a 6-week treatment with triiodothyronine (T3; daily injections of 3 or 6 μg/100 g body weight) or GC-1 (equimolar doses) on different metabolic parameters in adult female rats. Whereas all animals gained weight (17–25 g) in a way not basically affected by T3 or GC-1 treatment, only T3 treatment selectively increased food intake (50–70%). Oxygen consumption was significantly and equally increased (50–70%) by T3 and GC-1. Analysis of body composition by dual-energy X-ray absorptiometry (DEXA) revealed that, whereas control animals gained about 80% of fat mass, T3- or GC-1-treated animals lost 70–90 and ~20% respectively. Direct analysis of the carcass showed that T3 treatment promoted a 14–74% decrease in fat content but GC-1 treatment promoted only a 15–23% reduction. The gain in lean mass by DEXA and the carcass protein content were not affected by T3 or GC-1 treatment. However, the mass of individual skeletal muscles was negatively affected by T3 but only barely by GC-1. These findings highlight the potential use of GC-1 for the treatment of obesity and the metabolic syndrome.
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Two selective TH mimetics, GC-1 and KB141, can promote fat loss in rodents without causing unwanted effects on heart or muscle.
“Indeed, two of the selective TH mimetics, GC-1 and KB141, can promote fat loss in rodents without causing unwanted effects on heart or muscle 145,146.”
From Cellular bioenergetics as a target for obesity therapy (2010) · cites this paper as [145]
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- Authors
- Villicev, C. M., Freitas, F. R. S., Aoki, M. S., Taffarel, C., Scanlan, T. S., Moriscot, A. S., Ribeiro, M. O., Bianco, A. C., & Gouveia, C. H. A.
- Affiliations
- Universidade de São Paulo (BR)
- University of California, San Francisco (US)
- Universidade Presbiteriana Mackenzie (BR)
- Brigham and Women's Hospital (US)
- ORCID
- Venue
- Journal of Endocrinology
- Publisher
- Bioscientifica
- Published
- 2007-04
- Volume
- 193
- Issue
- 1
- Pages
- 21-29
- ISSN
- 0022-0795 (ISSN-L)
- 1479-6805
- OpenAlex
- W2115333838
- Cited by
- 120
- References
- 53
- Citations by year
- 2025: 4 · 2024: 5 · 2023: 3 · 2022: 2 · 2021: 5 · 2020: 1 · 2019: 3 · 2018: 3 · 2017: 9 · 2016: 9 · 2015: 4 · 2014: 12 · 2013: 12 · 2012: 4
- FWCI
- 8.77
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- Journal of Endocrinology (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Universidade de São Paulo
- Topics
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Thyroid Disorders and Treatments
- Life Sciences › Neuroscience › Endocrine and Autonomic Systems › Regulation of Appetite and Obesity
- Health Sciences › Medicine › Physiology › Adipose Tissue and Metabolism
- Keywords
- GC-1, thyroid hormone receptor beta, thyromimetics, triiodothyronine, energy expenditure, oxygen consumption, fat mass, body composition, obesity, metabolic syndrome, dietary intake, skeletal muscle mass, lean body mass
- MeSH terms
- Acetates, Adipose Tissue, Animals, Body Composition, Energy Metabolism, Female, Heart, Obesity, Organ Size, Oxygen Consumption, Phenols, Random Allocation, Triiodothyronine, Absorptiometry, Photon, Rats, Wistar, Muscle, Skeletal, Thyroid Hormone Receptors beta, Rats
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