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

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.

journal_name

Pharmacology

journal_title

Pharmacology

authors

Yang Y,Fu A,Wu X,Reagan JD

doi

10.1159/000335127

subject

Has Abstract

pub_date

2012-01-01 00:00:00

pages

13-7

issue

1-2

eissn

0031-7012

issn

1423-0313

pii

000335127

journal_volume

89

pub_type

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