期刊
PHARMACOLOGY
卷 82, 期 4, 页码 245-249出版社
KARGER
DOI: 10.1159/000157625
关键词
GPR35; G-protein-coupled receptors; 5-Nitro-2-(3-phenylpropylamino)benzoic acid; Zaprinast
GPR35 is a G(i/o)- and G(16)-coupled receptor abundantly expressed in gastrointestinal tissues and immune cells. Kynurenic acid (a tryptophan metabolite and ionotropic glutamate receptor antagonist) and zaprinast (a phosphodiesterase inhibitor) are GPR35 agonists. Here, we show that the chloride channel blocker 5-nitro-2-(3-phenylpropylamino) benzoic acid (NPPB) is also a GPR35 agonist. NPPB activates the GPR35-G(i/o) and GPR35-G(16) pathways in human embryonic kidney 293 (HEK293) cells and induces intracellular calcium mobilization in a concentration-dependent manner in HEK293 cells coexpressing human, rat or mouse GPR35 and the chimeric G protein G(qi5). These results suggest a novel pharmacological activity of NPPB and will provide useful information to search for more potent and selective GPR35 agonists. Copyright (C) 2008 S. Karger AG, Basel.
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