GPBA is a G-protein coupled receptor, also known as TGR5 or GPR131. Stimulation of the receptor with bile acids or other ligands induces the production of intracellular cAMP, activation of a MAP kinase signaling pathway and internalization of the receptor. Quantitative analyses for TGR5 mRNA have shown that it is abundantly expressed in monocytes/macrophages. The receptor is an attractive therapeutic target for the prevention and treatment of obesity and is highly associated with Type II diabetes and metabolic syndrome. GPBA has been implicated in inflammatory diseases, regulation of homeostasis by bile acids, as well as cardiovascular, neurological, and hepatic diseases.