TM-N1324

TM-N1324 also known as Cpd1324 is an agonist of GPR39, a G-protein-coupled receptor activated by Zn2+. GPR39 is a member of the ghrelin receptor family that has been implicated in the control of glucose-induced insulin secretion, pancreatic β-cell differentiation, control of lipolysis in white adipose tissue, and may also be involved in the pathophysiology of depression. TM-N1324 is found to activate human GPR39 with potencies of 280 nM and 9 nM in the absence and presence of Zn2+, respectively, and murine GPR39 with potencies of 180 nM and 5 nM in the absence and presence of Zn2+. TM-N1324 is known to stimulate gastric somatostatin secretion, indirectly inhibiting ghrelin secretion. It shows no agonist activity for 156 other GPCRs tested or for related receptors ghrelin and motilin. TM-N1324 serves as a tool to explore the physiological function of GPR39. It stimulates GLP-1 secretion in metabolic studies.