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Effect of a Low-Molecular-Weight Allosteric Agonist of the Thyroid-Stimulating Hormone Receptor on Basal and Thyroliberin-Stimulated Activity of Thyroid System in Diabetic Rats.
Int J Mol Sci
January 2025
Sechenov Institute of Evolutionary Physiology and Biochemistry, Russian Academy of Sciences, St. Petersburg 194223, Russia.
The approaches to correct thyroid deficiency include replacement therapy with thyroid hormones (THs), but such therapy causes a number of side effects. A possible alternative is thyroid-stimulating hormone (TSH) receptor activators, including allosteric agonists. The aim of this work was to study the effect of ethyl-2-(4-(4-(5-amino-6-(-butylcarbamoyl)-2-(methylthio)thieno[2,3-d]pyrimidin-4-yl)phenyl)--1,2,3-triazol-1-yl) acetate (TPY3m), a TSH receptor allosteric agonist developed by us, on basal and thyroliberin (TRH)-stimulated TH levels and the hypothalamic-pituitary-thyroid (HPT) axis in male rats with high-fat diet/low-dose streptozotocin-induced type 2 diabetes mellitus (T2DM).
View Article and Find Full Text PDFLow-molecular-weight Ligand of the Thyroid-stimulating Hormone Receptor with the Activity of a Partial Agonist and a Negative Allosteric Modulator.
Dokl Biochem Biophys
January 2025
I.M. Sechenov Institute of Evolutionary Physiology and Biochemistry, Russian Academy of Sciences, St. Petersburg, Russia.
Graves' disease is caused by overactivation of the thyroid-stimulating hormone receptor (TSHR). One approach for its treatment may be the use of negative allosteric modulators (NAM) of TSHR, which normalize TSHR activity and do not cause thyroid hormone (TH) deficiency. The aim of the work was to study the effect of a new compound 5-amino-4-(4-bromophenyl)-2-(methylthio)thieno[2,3-d]pyrimidine-6-carboxylic acid N-tert-butylamide (TPY4) on the basal and TSH-stimulated TH production in cultured FRTL-5 thyrocytes and on basal and thyrotropin-releasing hormone (TRH)-stimulated TH levels in the blood of rats.
View Article and Find Full Text PDFEctopic Thyrotropin-Secreting Tumor in the Nasopharynx Causing Central Hyperthyroidism.
JCEM Case Rep
January 2025
Section of Endocrinology and Investigative Medicine, Department of Metabolism, Digestion and Reproduction, Imperial College, London W12 ONN, UK.
We report a 31-year-old man with diarrhea and tachycardia. Diagnostic workup confirmed raised free thyroid hormones with unsuppressed thyroid stimulating hormone (TSH). Laboratory assay and medication interference were excluded.
View Article and Find Full Text PDFImmunization with OPN5 increased seasonal degradation of reproductive activity in Magang ganders.
Poult Sci
January 2025
College of Animal Science and Technology, Hunan Agricultural University, Changsha 410128, China. Electronic address:
To investigate the regulatory mechanism mediated by hypothalamic OPN5 on seasonal changes in the reproductive activities of domestic geese, 60 Magang ganders in their breeding period were selected for the experiment and evenly divided into an immunization group(OPN5-IM) and a control group. On days 0, 15 and 30, ganders in the immunized group were immunized with OPN5-KLH protein vaccine, and ganders in the control were immunized with the same amount of blank emulsified vaccine. Additionally, 120 female geese were provided to stimulate the reproductive activities of male geese.
View Article and Find Full Text PDFRole of Thyrotropin-Releasing Hormone Stimulation Test and Autoantibody in 952 Subjects with Subclinical Hypothyroidism.
J Endocr Soc
November 2024
Division of Endocrinology and Metabolism, Department of Internal Medicine, Soonchunhyang University Hospital, Soonchunhyang University College of Medicine, Seoul 04401, Korea.
Context: Subclinical hypothyroidism (SCH) is characterized by elevated thyroid-stimulating hormone (TSH) levels and normal free thyroxine (fT4) levels. In upper normal TSH levels, thyrotropin-releasing hormone (TRH) stimulation test proved to be useful in identifying an exaggerated TSH response.
Objective: We aimed to evaluate the incidence and predictive ability of basal TSH, anti-thyroid peroxidase antibodies (TPOAb), and anti-thyroglobulin antibodies (TgAb) for exaggerated TRH stimulation test in SCH.
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