5-Nitro-2-(3-Phenylpropylamino)benzoic Acid Is a GPR35 Agonist
2008; Karger Publishers; Volume: 82; Issue: 4 Linguagem: Inglês
10.1159/000157625
ISSN1423-0313
AutoresYasuhito Taniguchi, Hiroko Tonai‐Kachi, Katsuhiro Shinjo,
Tópico(s)Phosphodiesterase function and regulation
ResumoGPR35 is a G<sub>i/o</sub>- and G<sub>16</sub>-coupled receptor abundantly expressed in gastrointestinal tissues and immune cells. Kynurenic acid (a tryptophan metabolite and ionotropic glutamate receptor antagonist) and zaprinast (a phosphodies- terase 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<sub>i/o</sub> and GPR35-G<sub>16</sub> 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<sub>qi5</sub>. These results suggest a novel pharmacological activity of NPPB and will provide useful information to search for more potent and selective GPR35 agonists.
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