ArticleDrug design, development and therapy2017
Investigation of triamterene as an inhibitor of the TGR5 receptor: identification in cells and animals.
Article in Drug design, development and therapy, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 30 citations in OpenAlex.
- Gut-Brain Axis and Bile Acid Signaling: Linking Microbial Metabolism to Brain Function and Metabolic Regulation.International journal of molecular sciences · 2025Review
- Taurodeoxycholic, taurocholic, and glycocholic acids promote hepatic gluconeogenesis via TGR5 in dairy cows.Journal of animal science and biotechnology · 2025Article
- Increase in bile acids after sleeve gastrectomy improves metabolism by activating GPBAR1 to increase cAMP in mice with nonalcoholic fatty liver disease.Immunity, inflammation and disease · 2024Article
- The function of the gut microbiota-bile acid-TGR5 axis in diarrhea-predominant irritable bowel syndrome.mSystems · 2024Article
- Identification of Andrographolide as an Agonist of Bile Acid TGR5 Receptor in a Cell Line to Demonstrate the Reduction in Hyperglycemia in Type-1 Diabetic Rats.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Bile acid receptors and renal regulation of water homeostasis.Frontiers in physiology · 2023Review
- Drug-Drug Interactions in Vestibular Diseases, Clinical Problems, and Medico-Legal Implications.International journal of environmental research and public health · 2021Review
- Evolutionary metabolic landscape from preneoplasia to invasive lung adenocarcinoma.Nature communications · 2021Article
- TGR5 Expression Is Associated with Changes in the Heart and Urinary Bladder of Rats with Metabolic Syndrome.Life (Basel, Switzerland) · 2021Article
- Triamterene induces autophagic degradation of lysosome by exacerbating lysosomal integrity.Archives of pharmacal research · 2021Article
- Finger Citron Extract Ameliorates Glycolipid Metabolism and Inflammation by Regulating GLP-1 Secretion via TGR5 Receptors in Obese Rats.Evidence-based complementary and alternative medicine : eCAM · 2021Article
- Simulating the Post-gastric Bypass Intestinal Microenvironment Uncovers a Barrier-Stabilizing Role for FXR.iScience · 2020Article
- TGR5 Signaling in Hepatic Metabolic Health.Nutrients · 2020Review
- Compound 18 Improves Glucose Tolerance in a Hepatocyte TGR5-dependent Manner in Mice.Nutrients · 2020Article
- The influence of the host microbiome on 3,4-methylenedioxymethamphetamine (MDMA)-induced hyperthermia and vice versa.Scientific reports · 2019Article
- TGR5 activation ameliorates hyperglycemia-induced cardiac hypertrophy in H9c2 cells.Scientific reports · 2019Article
- The Dietary Furocoumarin Imperatorin Increases Plasma GLP-1 Levels in Type 1-Like Diabetic Rats.Nutrients · 2017Article
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundG-protein-coupled bile acid receptor 1 (GPBAR1, also known as TGR5) has been shown to participate in glucose homeostasis. In animal models, a TGR5 agonist increases incretin secretion to reduce hyperglycemia. Many agonists have been developed for clinical use. However, the effects of TGR5 blockade have not been studied extensively, with the exception of studies using TGR5 knockout mice. Therefore, we investigated the potential effect of triamterene on TGR5.
methodsWe transfected the TGR5 gene into cultured Chinese hamster ovary cells (CHO-K1 cells) to express TGR5. Then, we applied a fluorescent indicator to examine the glucose uptake of these transfected cells. In addition, NCI-H716 cells that secrete incretin were also evaluated. Fura-2, a fluorescence indicator, was applied to determine the changes in calcium concentrations. The levels of cyclic adenosine monophosphate (cAMP) and glucagon-like peptide (GLP-1) were estimated using enzyme-linked immunosorbent assay kits. Moreover, rats with streptozotocin (STZ)-induced type 1-like diabetes were used to investigate the effects in vivo.
resultsTriamterene dose dependently inhibits the increase in glucose uptake induced by TGR5 agonists in CHO-K1 cells expressing the TGR5 gene. In cultured NCI-H716 cells, TGR5 activation also increases GLP-1 secretion by increasing calcium levels. Triamterene inhibits the increased calcium levels by TGR5 activation through competitive antagonism. Moreover, the GLP-1 secretion and increased cAMP levels induced by TGR5 activation are both dose dependently reduced by triamterene. However, treatment with KB-R7943 at a dose sufficient to block the Na
conclusionBased on the obtained data, we identified triamterene as a reliable inhibitor of TGR5. Therefore, triamterene can be developed as a clinical inhibitor of TGR5 activation in future studies.
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