GPR35 Is a Target of the Loop Diuretic Drugs Bumetanide and Furosemide
| Autor: | Jeff D. Reagan, Xiaosu Wu, Angela Fu, Yuhua Yang |
|---|---|
| Rok vydání: | 2012 |
| Předmět: |
medicine.medical_specialty
medicine.drug_class Inositol Phosphates CHO Cells Pharmacology Transfection Receptors G-Protein-Coupled Mice Furosemide Cricetinae Internal medicine Calcium flux medicine Animals Humans Diuretics Inositol phosphate Receptor Bumetanide Skin chemistry.chemical_classification General Medicine Chlorothiazide Loop diuretic Rats HEK293 Cells Hydrochlorothiazide Endocrinology chemistry Calcium Cotransporter HT29 Cells medicine.drug |
| Zdroj: | Pharmacology. 89:13-17 |
| ISSN: | 1423-0313 0031-7012 |
| DOI: | 10.1159/000335127 |
| Popis: | We report that the loop diuretic drugs bumetanide and furosemide used in the treatment of hypertension are GPR35 agonists. We utilized calcium flux, inositol phosphate accumulation, and dynamic redistribution assays to examine the pharmacology of these compounds on the human, mouse and rat GPR35. While potent on human GPR35, neither bumetanide nor furosemide were active against mouse or rat GPR35. Furthermore, the Na+-Cl– cotransporter inhibi- tors chlorothiazide and hydrochlorothiazide were inactive against GPR35 in all three species. We also demonstrate that GPR35 is expressed in human skin where it has been shown that loop diuretics inhibit histamine-induced flare and itch response. These findings suggest that GPR35 may play an important role in skin cell biology and be a potential target for the treatment of a variety of immune disorders. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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