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J.Health Sci., 55(1), 132-137, 2009

Inhibitory Effect of Relaxin-3 on Insulin Secretion in Isolated Pancreas and Insulinoma

Hiroyuki Yamamoto,* Takeo Arai, Ryota Tasaka, Yasunori Mori, Kazuaki Iguchi, Keiko Unno, and Minoru Hoshino

Laboratory of Bioorganic Chemistry, School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Shizuoka 422-8526, Japan

Relaxin-3 is a recently discovered member of the insulin superfamily and is a ligand for three orphan G-protein-coupled receptors: GPCR135, GPCR142 and LGR7 (leucine-rich repeat-containing G-protein-coupled receptor 7). GPCR135 mRNA is expressed in the pancreas, however, it is not known, whether the peptide affects pancreatic islet function. Reverse transcriptase (RT)-PCR and radioreceptor assay have shown that the relaxin-3 receptor (GPCR135) is expressed in pancreatic islets and rat insulinoma, but LGR7 is not expressed. Moreover, relaxin-3 has been revealed to inhibit the secretion of insulin from pancreatic islets. However, we can not detect relaxin-3 in small intestine and pancreas. These results suggest a novel role of relaxin-3 in the regulation of insulin release.