Insulinotropic activity of the imidazoline derivative RX871024 in the diabetic GK rat

Alexander M. Efanov, Ioulia B. Appelskog, Samy M. Abdel-Halim, Akhtar Khan, Robert Bränström, Olof Larsson, Claes Göran Östenson, Hans Juergen Mest, Per Olof Berggren, Suad Efendic, Sergei V. Zaitsev

Research output: Contribution to journalArticlepeer-review

12 Scopus citations


The insulinotropic activity of the imidazoline derivative RX871024 was compared in pancreatic islets from nondiabetic Wistar rats and spontaneously diabetic Goto-Kakizaki (GK) rats. RX871024 significantly stimulated insulin secretion in islets from both animal groups. The insulinotropic activity of RX871024 was higher than that of the sulfonylurea glibenclamide. This difference was more pronounced in islets from GK rats compared with Wistar rat islets. More importantly, RX871024 substantially improved glucose sensitivity in diabetic β-cells, whereas glibenclamide stimulated insulin secretion about twofold over a broad range of glucose concentrations in nondiabetic and diabetic rats. RX871024 induced a faster increase in cytosolic free Ca2+ concentration and faster inhibition of ATP-dependent K+ channel activity in GK rat islets compared with Wistar rat islets. RX871024 also induced a more pronounced increase in diacylglycerol concentration in GK rat islets. These data support the idea that imidazoline compounds can form the basis for the development of novel drugs for treatment of type 2 diabetes, which can restore glucose sensitivity in diabetic β-cells.

Original languageEnglish (US)
Pages (from-to)E117-E124
JournalAmerican Journal of Physiology - Endocrinology and Metabolism
Issue number1 45-1
StatePublished - 2002
Externally publishedYes


  • Diabetic rats
  • Imidazolines
  • Insulin secretion
  • Pancreatic islets

ASJC Scopus subject areas

  • Physiology
  • Endocrinology
  • Biochemistry


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