Ay-4166 increases the sensitivity of insulin secretion to glucose in isolated perfused rat pancreas.

To study the effect of a therapeutic dose (3 microM) of AY-4166 on the glucose-stimulated insulin secretion, the rat pancreas was perfused with 5 to 15 mM glucose. AY-4166 did not affect the basal insulin secretion at 5 mM glucose, and increased the first and second phases of insulin secretion stimulated by 7.5 to 15 mM glucose. The dose-response curve of the insulin secretion to glucose was shifted to the left side by AY-4166. These results suggest that AY-4166 ist not a stimulator releasing insulin independently of glucose concentrations, but a potentiator of insulin secretion.