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编 号：F236698
分子式：C13H14N2O
分子量：214.26
分子式：C13H14N2O
分子量：214.26
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CAS No: 189224-48-4
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KU14R is a new I(3)-R antagonist, which selectively blocks the insulin secretory response to imidazolines.IC50 Value:Target: Insulin ReceptorA 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. KU14R partially attenuated responses to Imidazole-4-acetic acid-ribotide (IAA-RP). The effects of KU14R on stimulus secretion-coupling in normal mouse islets and beta cells was compared by measuring KATP channel activity, plasma membrane potential, cytosolic calcium concentration ([Ca2+]c) and dynamic insulin secretion. In the presence of 10 mmol/l but not of 5 mmol/l glucose, KU14R (30, 100 or 300 micromol/l) was ineffective. 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.
KU14R is a new I(3)-R antagonist, which selectively blocks the insulin secretory response to imidazolines.IC50 Value:Target: Insulin ReceptorA 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. KU14R partially attenuated responses to Imidazole-4-acetic acid-ribotide (IAA-RP). The effects of KU14R on stimulus secretion-coupling in normal mouse islets and beta cells was compared by measuring KATP channel activity, plasma membrane potential, cytosolic calcium concentration ([Ca2+]c) and dynamic insulin secretion. In the presence of 10 mmol/l but not of 5 mmol/l glucose, KU14R (30, 100 or 300 micromol/l) was ineffective. 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.
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