Abstract: The glucagons-like peptide-1 (GLP-1) is an effective anti-hyperglycemic endogenous hormone which is mainly produced in the intestinal L cells. GLP-1 can promotes glucose-dependent insulin secretion and inhibits glucagon release, however, endogenous GLP-1 has a short half-life of less than 2 min and can be easily degraded by dipeptidyl peptidase-4 (DPP4). The currently developed GLP-1 analogs such as exenatide and liraglutide can prolong the half-life while maintaining its biological activity. It is reported that GLP-1 receptor (GLP-1R) is highly expressed on the surface of pancreatic β-cells and insulinoma. Therefore, GLP-1 and its analogs labeled with radionuclides are currently a popular class of molecular probes for the diagnosis and treatment of insulinoma, quantification and functional assessment of pancreatic β-cells, and in vivo tracking of transplanted islets. As more physiological and pharmacological effects of GLP-1 and its analogs are revealed in vivo, the use of such probes in diseases including cardiovascular diseases and neuropsychiatric disorders is gradually becoming possible. This review mainly summarized the research progress of radiolabeled GLP-1 and its analogs targeting GLP-1 receptors in insulinoma and pancreatic β-cells. In addition, we further combined the physiological role of GLP-1 to prospect the future development of radiolabeled GLP-1 and its analogs in more fields.