Effects of the hypoglycaemic drugs repaglinide and glibenclamide on ATP-sensitive potassium-channels and cytosolic calcium levels in beta TC3 cells and rat pancreatic beta cells

Diabetologia
J GromadaJ Frøkjaer-Jensen

Abstract

The present study demonstrates the action of the hypoglycaemic drugs repaglinide and glibenclamide in cultured newborn rat islet cells and mouse beta TC3 cells. In cell-attached membrane patches of newborn rat islet cells repaglinide (10 nmol/l) and glibenclamide (20 nmol/l) decrease the open probability of single ATP-sensitive K(+)-channels to approximately 10% of the activity prior to addition of the drugs in short-term experiments (< 5 min). The influence of repaglinide and glibenclamide on the ATP-sensitive K+ current was studied using the whole-cell patch clamp configuration. A half-maximal steady-state inhibition of the ATP-sensitive K+ currents is observed at 89 pmol/l repaglinide and at 47 pmol/l glibenclamide in whole-cell experiments of longer duration (30 min). Applying digital Ca2+ imaging on single beta TC3 cells we found that repaglinide and glibenclamide induced a concentration-dependent increase in intracellular free Ca2+ concentration ([Ca2+]i) with a half-maximal effect at 0.5 nmol/l for both drugs in long-term experiments (30 min). The rise in [Ca2+]i results from Ca2+ entry through voltage-dependent L-type Ca(2+)-channels since it is inhibited by verapamil (10 mumol/l). The effect of repaglinide and glibencl...Continue Reading

References

Dec 1, 1992·Hormone and Metabolic Research = Hormon- Und Stoffwechselforschung = Hormones Et Métabolisme·U PantenC Schwanstecher
Dec 15, 1992·Biochimica Et Biophysica Acta·S J Ashcroft, F M Ashcroft
Jun 1, 1992·Diabetes Care·L C Groop
Nov 1, 1986·Pflügers Archiv : European journal of physiology·G TrubeT Ohno-Shosaku
Jul 15, 1987·Biochemical and Biophysical Research Communications·H Schmid-AntomarchiM Lazdunski
Jan 1, 1988·Annual Review of Neuroscience·F M Ashcroft
Jan 1, 1989·Progress in Biophysics and Molecular Biology·F M Ashcroft, P Rorsman
Jan 1, 1989·Molecular Endocrinology·J H NielsenO D Madsen
Nov 2, 1989·The New England Journal of Medicine·J E Gerich
Sep 1, 1989·Naunyn-Schmiedeberg's Archives of Pharmacology·B J ZünklerU Panten
Dec 1, 1988·Proceedings of the National Academy of Sciences of the United States of America·S EfratS Baekkeskov
Apr 1, 1986·Diabetologia·J L CarpentierW J Malaisse
Apr 1, 1994·Diabetes/metabolism Reviews·A E PontiroliG Pozza
Jan 1, 1993·European Journal of Clinical Pharmacology·B H WolffenbuttelA C Kruseman

❮ Previous
Next ❯

Citations

Nov 16, 2011·Naunyn-Schmiedeberg's Archives of Pharmacology·Petra KühnerUlrich Quast
Jun 8, 2001·Clinical Therapeutics·J E Gerich
Jun 16, 1999·Diabetes Research and Clinical Practice·T MarburyH Lebovitz
Jun 4, 1999·Drug Discovery Today·H Shinkai
Aug 1, 1997·British Journal of Pharmacology·M Mark, W Grell
Jan 1, 2009·Diabetes, Metabolic Syndrome and Obesity : Targets and Therapy·Robert Moses
Jun 27, 2002·Clinical Pharmacokinetics·Vibeke Hatorp
Oct 24, 2007·American Journal of Cardiovascular Drugs : Drugs, Devices, and Other Interventions·Odd Erik Johansen, Kåre I Birkeland
Jun 12, 2009·Drug Metabolism Reviews·Shu-Feng ZhouBalram Chowbay
Dec 18, 2012·Expert Opinion on Drug Safety·Stephanie Aleskow SteinStephen N Davis
Aug 1, 1997·Expert Opinion on Investigational Drugs·B E Dunning
Sep 15, 2009·Best Practice & Research. Clinical Endocrinology & Metabolism·M Nauck, U Smith
Jan 29, 2005·British Journal of Pharmacology·Ann Maria K HansenPhilip Wahl
Aug 16, 2003·British Journal of Clinical Pharmacology·Tanja Busk BidstrupKristian Tage Hansen
Feb 21, 2008·The Journal of Pharmacy and Pharmacology·Naveen KumarAshok Kumar Tiwary
Sep 20, 2011·Diabetes, Obesity & Metabolism·A S AbdelmoneimS H Simpson
Jun 3, 2011·Clinical and Experimental Pharmacology & Physiology·Fei-Feng ShengZhao-Qian Liu
May 18, 2004·European Journal of Pharmacology·Yang ZhangDavid S Roane
Nov 4, 2000·Expert Opinion on Investigational Drugs·M Massi-Benedetti, P Damsbo
Feb 24, 2015·Journal of Ethnopharmacology·Jia CuiAi-Dong Wen
Dec 3, 1999·Biochimica Et Biophysica Acta·J Bryan, L Aguilar-Bryan
Jun 19, 2013·The Korean Journal of Physiology & Pharmacology : Official Journal of the Korean Physiological Society and the Korean Society of Pharmacology·Chong-Ki LeeJoon Seok Bang
May 27, 2004·Diabetes Care·Julio RosenstockUNKNOWN Repaglinide Versus Nateglinide Comparison Study Group

❮ Previous
Next ❯

Related Concepts

Related Feeds