KU14R is a novel I(3)-R antagonist that selectively inhibits the insulin secretory response to imidazolines.

KU14R partially attenuated responses to Imidazole-4-acetic acid-ribotide (IAA-RP). Insulin Receptor A new I(3)-R antagonist, KU14R (2 (2-ethyl 2,3-dihydro-2-benzofuranyl)-2-imidazole), which selectively blocks the insulin secretory response to imidazolines. By measuring KATP channel activity, plasma membrane potential, cytosolic calcium concentration ([Ca2+]c), and dynamic insulin secretion to compare the effects of KU14R on stimulus secretion-coupling in normal mouse islets and beta cells. KU14R (30, 100 or 300 micromol/l) was ineffective, in the presence of 10 mmol/l but not of 5 mmol/l glucose. KATP channel was blocked by KU14R (IC50 31.9 micromol/l, Hill slope -1.5). KU14R does not act as an antagonist of either efaroxan or S22068 at an imidazoline site in vivo.