The imidazoline RX871024 stimulates insulin secretion in pancreatic β-cells from mice deficient in KAPT channel function

Alexander M. Efanov, Marianne Hoy, Robert Bränström, Sergei V. Zaitsev, Mark A. Magnuson, Suad Efendic, Jesper Gromada, Per Olof Berggren

Research output: Contribution to journalArticle

15 Citations (Scopus)

Abstract

Effects of the imidazoline compound RX871024 on cytosolic free Ca2+ concentration ([Ca2+]i) and insulin secretion in pancreatic β-cells from SUR1 deficient mice have been studied. In β-cells from wild-type mice RX871024 increased [Ca2+]i by blocking ATP-dependent K+-current (KATP) and inducing membrane depolarization. In β-cells lacking a component of the KATP-channel, SUR1 subunit, RX871024 failed to increase [Ca2+]i. However, insulin secretion in these cells was strongly stimulated by the imidazoline. Thus, a major component of the insulinotropic activity of RX871024 is stimulation of insulin exocytosis independently from changes in KATP-current and [Ca2+]i. This means that effects of RX871024 on insulin exocytosis are partly mediated by interaction with proteins distinct from those composing the KATP-channel.

Original languageEnglish
Pages (from-to)918-922
Number of pages5
JournalBiochemical and Biophysical Research Communications
Volume284
Issue number4
DOIs
StatePublished - Oct 14 2001
Externally publishedYes

Fingerprint

Imidazolines
Insulin
KATP Channels
Exocytosis
Depolarization
Adenosine Triphosphate
2-(2-imidazolin-2-yl)-1-phenyl-1H-indole
Membranes
Proteins

Keywords

  • ATP-dependent K-channel
  • Cytosolic free Ca concentration
  • Imidazoline
  • Insulin secretion

ASJC Scopus subject areas

  • Biochemistry
  • Biophysics
  • Molecular Biology

Cite this

The imidazoline RX871024 stimulates insulin secretion in pancreatic β-cells from mice deficient in KAPT channel function. / Efanov, Alexander M.; Hoy, Marianne; Bränström, Robert; Zaitsev, Sergei V.; Magnuson, Mark A.; Efendic, Suad; Gromada, Jesper; Berggren, Per Olof.

In: Biochemical and Biophysical Research Communications, Vol. 284, No. 4, 14.10.2001, p. 918-922.

Research output: Contribution to journalArticle

Efanov, AM, Hoy, M, Bränström, R, Zaitsev, SV, Magnuson, MA, Efendic, S, Gromada, J & Berggren, PO 2001, 'The imidazoline RX871024 stimulates insulin secretion in pancreatic β-cells from mice deficient in KAPT channel function', Biochemical and Biophysical Research Communications, vol. 284, no. 4, pp. 918-922. https://doi.org/10.1006/bbrc.2001.5068
Efanov, Alexander M. ; Hoy, Marianne ; Bränström, Robert ; Zaitsev, Sergei V. ; Magnuson, Mark A. ; Efendic, Suad ; Gromada, Jesper ; Berggren, Per Olof. / The imidazoline RX871024 stimulates insulin secretion in pancreatic β-cells from mice deficient in KAPT channel function. In: Biochemical and Biophysical Research Communications. 2001 ; Vol. 284, No. 4. pp. 918-922.
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