GPR35 is a target of the loop diuretic drugs bumetanide and furosemide.

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Yang Y, Fu A, Wu X, Reagan JD

GPR35 is a target of the loop diuretic drugs bumetanide and furosemide.

Pharmacology. 2012;89(1-2):13-7. doi: 10.1159/000335127. Epub 2012 Jan 10.

PubMed ID

22236570 [ View in PubMed

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Abstract

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.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Furosemide	G-protein coupled receptor 35	Protein	Humans	Unknown	Agonist	Details