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. 1991 Jan;102(1):113–118. doi: 10.1111/j.1476-5381.1991.tb12141.x

Effects of glibenclamide on cytosolic calcium concentrations and on contraction of the rabbit aorta.

K Yoshitake 1, K Hirano 1, H Kanaide 1
PMCID: PMC1917894  PMID: 1904292

Abstract

1. Using fluorometry of fura-2 and rabbit aortic strips, we studied the effects of glibenclamide (GLB), a sulphonylurea anti-diabetic drug and an inhibitor of opening of K+ channels, on cytosolic calcium concentrations ([Ca2+]i) and on force development. 2. Both high K(+)-depolarization and noradrenaline (NA) increased [Ca2+]i and force, in a concentration-dependent manner, in the presence of extracellular Ca2+ (1.25 mM). However, force development in relation to [Ca2+]i ([Ca2+]i-force relationship) observed with NA was much greater than that observed with K(+)-depolarization. 3. Pretreatment with GLB (10(-6)-10(-4) M) for 10 min partially inhibited, in a concentration-dependent manner, both [Ca2+]i elevation and the force development induced by 118 mM K(+)-depolarization or NA 10(-5) M in the presence of extracellular Ca2+. The [Ca2+]i-force relationship induced by both 118 mM K+ physiological salt solutions and by NA 10(-5) M in the GLB-treated strips overlapped that obtained in the non-treated strips, thereby suggesting that GLB has no effect on the Ca2(+)-sensitivity of the intracellular contractile apparatus. Only high concentrations (10(-4) M) of GLB decreased [Ca2+]i and the force, when applied after the force induced by 118 mM K+ PSS or NA 10(-5) M reached the maximum level. 4. In the absence of extracellular Ca2+, NA induced a transient increase in [Ca2+]i and in the force and these increases were inhibited when the vascular strips were pretreated with GLB for 10 min. The [Ca2+]i-force relationship obtained in the GLB-treated strips overlapped that in the non-treated ones.(ABSTRACT TRUNCATED AT 250 WORDS)

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Selected References

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  1. Ashcroft F. M., Harrison D. E., Ashcroft S. J. Glucose induces closure of single potassium channels in isolated rat pancreatic beta-cells. 1984 Nov 29-Dec 5Nature. 312(5993):446–448. doi: 10.1038/312446a0. [DOI] [PubMed] [Google Scholar]
  2. Ashford M. L., Sturgess N. C., Trout N. J., Gardner N. J., Hales C. N. Adenosine-5'-triphosphate-sensitive ion channels in neonatal rat cultured central neurones. Pflugers Arch. 1988 Aug;412(3):297–304. doi: 10.1007/BF00582512. [DOI] [PubMed] [Google Scholar]
  3. Boyd A. E., 3rd Sulfonylurea receptors, ion channels, and fruit flies. Diabetes. 1988 Jul;37(7):847–850. doi: 10.2337/diab.37.7.847. [DOI] [PubMed] [Google Scholar]
  4. Doggrell S. A., Smith J. W., Downing O. A., qilson K. A. Hyperpolarizing action of cromakalim on the rat aorta. Eur J Pharmacol. 1989 Dec 12;174(1):131–133. doi: 10.1016/0014-2999(89)90885-6. [DOI] [PubMed] [Google Scholar]
  5. Findlay I., Dunne M. J., Petersen O. H. ATP-sensitive inward rectifier and voltage- and calcium-activated K+ channels in cultured pancreatic islet cells. J Membr Biol. 1985;88(2):165–172. doi: 10.1007/BF01868430. [DOI] [PubMed] [Google Scholar]
  6. Furchgott R. F., Zawadzki J. V. The obligatory role of endothelial cells in the relaxation of arterial smooth muscle by acetylcholine. Nature. 1980 Nov 27;288(5789):373–376. doi: 10.1038/288373a0. [DOI] [PubMed] [Google Scholar]
  7. Gaines K. L., Hamilton S., Boyd A. E., 3rd Characterization of the sulfonylurea receptor on beta cell membranes. J Biol Chem. 1988 Feb 25;263(6):2589–2592. [PubMed] [Google Scholar]
  8. Gerich J. E. Oral hypoglycemic agents. N Engl J Med. 1989 Nov 2;321(18):1231–1245. doi: 10.1056/NEJM198911023211805. [DOI] [PubMed] [Google Scholar]
  9. Grynkiewicz G., Poenie M., Tsien R. Y. A new generation of Ca2+ indicators with greatly improved fluorescence properties. J Biol Chem. 1985 Mar 25;260(6):3440–3450. [PubMed] [Google Scholar]
  10. Hirano K., Kanaide H., Nakamura M. Effects of okadaic acid on cytosolic calcium concentrations and on contractions of the porcine coronary artery. Br J Pharmacol. 1989 Dec;98(4):1261–1266. doi: 10.1111/j.1476-5381.1989.tb12672.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  11. Murphy R. A., Herlihy J. T., Megerman J. Force-generating capacity and contractile protein content of arterial smooth muscle. J Gen Physiol. 1974 Dec;64(6):691–705. doi: 10.1085/jgp.64.6.691. [DOI] [PMC free article] [PubMed] [Google Scholar]
  12. Noma A. ATP-regulated K+ channels in cardiac muscle. Nature. 1983 Sep 8;305(5930):147–148. doi: 10.1038/305147a0. [DOI] [PubMed] [Google Scholar]
  13. Okabe K., Kajioka S., Nakao K., Kitamura K., Kuriyama H., Weston A. H. Actions of cromakalim on ionic currents recorded from single smooth muscle cells of the rat portal vein. J Pharmacol Exp Ther. 1990 Feb;252(2):832–839. [PubMed] [Google Scholar]
  14. Petersen O. H., Findlay I. Electrophysiology of the pancreas. Physiol Rev. 1987 Jul;67(3):1054–1116. doi: 10.1152/physrev.1987.67.3.1054. [DOI] [PubMed] [Google Scholar]
  15. Pogátsa G., Dubecz E. The direct effect of hypoglycaemic sulphonylureas on myocardial contractile force and arterial blood pressure. Diabetologia. 1977 Sep;13(5):515–519. doi: 10.1007/BF01234506. [DOI] [PubMed] [Google Scholar]
  16. Rink T. J., Pozzan T. Using quin2 in cell suspensions. Cell Calcium. 1985 Apr;6(1-2):133–144. doi: 10.1016/0143-4160(85)90040-5. [DOI] [PubMed] [Google Scholar]
  17. Schmid-Antomarchi H., de Weille J., Fosset M., Lazdunski M. The antidiabetic sulfonylurea glibenclamide is a potent blocker of the ATP-modulated K+ channel in insulin secreting cells. Biochem Biophys Res Commun. 1987 Jul 15;146(1):21–25. doi: 10.1016/0006-291x(87)90684-x. [DOI] [PubMed] [Google Scholar]
  18. Spruce A. E., Standen N. B., Stanfield P. R. Voltage-dependent ATP-sensitive potassium channels of skeletal muscle membrane. Nature. 1985 Aug 22;316(6030):736–738. doi: 10.1038/316736a0. [DOI] [PubMed] [Google Scholar]
  19. Standen N. B., Quayle J. M., Davies N. W., Brayden J. E., Huang Y., Nelson M. T. Hyperpolarizing vasodilators activate ATP-sensitive K+ channels in arterial smooth muscle. Science. 1989 Jul 14;245(4914):177–180. doi: 10.1126/science.2501869. [DOI] [PubMed] [Google Scholar]
  20. Sturgess N. C., Ashford M. L., Cook D. L., Hales C. N. The sulphonylurea receptor may be an ATP-sensitive potassium channel. Lancet. 1985 Aug 31;2(8453):474–475. doi: 10.1016/s0140-6736(85)90403-9. [DOI] [PubMed] [Google Scholar]
  21. Tsien R. Y., Pozzan T., Rink T. J. Calcium homeostasis in intact lymphocytes: cytoplasmic free calcium monitored with a new, intracellularly trapped fluorescent indicator. J Cell Biol. 1982 Aug;94(2):325–334. doi: 10.1083/jcb.94.2.325. [DOI] [PMC free article] [PubMed] [Google Scholar]
  22. Villar A., D'Ocon M. P., Anselmi E. Relaxant effects of sulfonylureas on induced contractions of rat uterine smooth muscle: role of intracellular calcium. Arch Int Pharmacodyn Ther. 1986 Feb;279(2):248–257. [PubMed] [Google Scholar]

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