Two generations of insulinotropic imidazoline compounds.

  title={Two generations of insulinotropic imidazoline compounds.},
  author={Suad Efend{\'i}c and Alexander M. Efanov and P. -O. Berggren and Sergei V. Zaitsev},
  volume={51 Suppl 3},
The imidazoline RX871024 increased basal- and glucose-stimulated insulin release in vitro and in vivo. The compound inhibited activity of ATP-sensitive K(+) channels as well as voltage-gated K(+) channels, which led to membrane depolarization, an increase in the cytosolic Ca(2+) concentration ([Ca(2+)](i)), and insulin release. Importantly, RX871024 also enhanced the insulinotropic effect of glucose in cells with clamped [Ca(2+)](i) but in the presence of high ATP and Ca(2+)concentration inside… CONTINUE READING
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