Skip to main content
NCBI home page
British Journal of Pharmacology logoLink to British Journal of Pharmacology
. 1992 Sep;107(1):152–155. doi: 10.1111/j.1476-5381.1992.tb14478.x

Effects of cromakalim on the membrane potassium permeability of frog skeletal muscle in vitro.

D C Benton 1, D G Haylett 1
PMCID: PMC1907595  PMID: 1422569

Abstract

1. The effects of the potassium channel opener, cromakalim, and its active enantiomer, lemakalim, have been investigated in frog skeletal muscle. 2. Cromakalim (30-300 microM) increased 86Rb efflux from muscles loaded with the isotope, hyperpolarized the fibres and reduced membrane resistance. 3. These effects were inhibited by the sulphonylureas, glibenclamide and tolbutamide. The IC50 for glibenclamide inhibition of 86Rb efflux was ca. 8 nM. 4. Phentolamine (300 microM) (which blocks responses to cromakalim in smooth muscle and inhibits ATP-sensitive K+ channels in pancreatic beta-cells) had no effect on the reduction in membrane resistance caused by 100 microM lemakalim. 5. Diazoxide (600 microM) had no effect on 86Rb efflux. 6. The similarities of the K+ channel activated by cromakalim in frog skeletal muscle to the channel acted on in smooth muscle and to the ATP-sensitive K+ channel of beta-cells are discussed.

Full text

PDF
152

Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Ashcroft F. M. Adenosine 5'-triphosphate-sensitive potassium channels. Annu Rev Neurosci. 1988;11:97–118. doi: 10.1146/annurev.ne.11.030188.000525. [DOI] [PubMed] [Google Scholar]
  2. Castle N. A., Haylett D. G. Effect of channel blockers on potassium efflux from metabolically exhausted frog skeletal muscle. J Physiol. 1987 Feb;383:31–43. doi: 10.1113/jphysiol.1987.sp016394. [DOI] [PMC free article] [PubMed] [Google Scholar]
  3. Dunne M. J., Aspinall R. J., Petersen O. H. The effects of cromakalim on ATP-sensitive potassium channels in insulin-secreting cells. Br J Pharmacol. 1990 Jan;99(1):169–175. doi: 10.1111/j.1476-5381.1990.tb14672.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  4. Dunne M. J. Block of ATP-regulated potassium channels by phentolamine and other alpha-adrenoceptor antagonists. Br J Pharmacol. 1991 Aug;103(4):1847–1850. doi: 10.1111/j.1476-5381.1991.tb12340.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  5. Escande D., Thuringer D., Leguern S., Cavero I. The potassium channel opener cromakalim (BRL 34915) activates ATP-dependent K+ channels in isolated cardiac myocytes. Biochem Biophys Res Commun. 1988 Jul 29;154(2):620–625. doi: 10.1016/0006-291x(88)90184-2. [DOI] [PubMed] [Google Scholar]
  6. Faivre J. F., Findlay I. Effects of tolbutamide, glibenclamide and diazoxide upon action potentials recorded from rat ventricular muscle. Biochim Biophys Acta. 1989 Aug 21;984(1):1–5. doi: 10.1016/0005-2736(89)90334-9. [DOI] [PubMed] [Google Scholar]
  7. Fink R., Hase S., Lüttgau H. C., Wettwer E. The effect of cellular energy reserves and internal calcium ions on the potassium conductance in skeletal muscle of the frog. J Physiol. 1983 Mar;336:211–228. doi: 10.1113/jphysiol.1983.sp014577. [DOI] [PMC free article] [PubMed] [Google Scholar]
  8. Fink R., Lüttgau H. C. An evaluation of the membrane constants and the potassium conductance in metabolically exhausted muscle fibres. J Physiol. 1976 Dec;263(2):215–238. doi: 10.1113/jphysiol.1976.sp011629. [DOI] [PMC free article] [PubMed] [Google Scholar]
  9. Garrino M. G., Plant T. D., Henquin J. C. Effects of putative activators of K+ channels in mouse pancreatic beta-cells. Br J Pharmacol. 1989 Nov;98(3):957–965. doi: 10.1111/j.1476-5381.1989.tb14626.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  10. Hamilton T. C., Weston A. H. Cromakalim, nicorandil and pinacidil: novel drugs which open potassium channels in smooth muscle. Gen Pharmacol. 1989;20(1):1–9. doi: 10.1016/0306-3623(89)90052-9. [DOI] [PubMed] [Google Scholar]
  11. Hodgkin A. L., Nakajima S. The effect of diameter on the electrical constants of frog skeletal muscle fibres. J Physiol. 1972 Feb;221(1):105–120. doi: 10.1113/jphysiol.1972.sp009742. [DOI] [PMC free article] [PubMed] [Google Scholar]
  12. Hof R. P., Quast U., Cook N. S., Blarer S. Mechanism of action and systemic and regional hemodynamics of the potassium channel activator BRL34915 and its enantiomers. Circ Res. 1988 Apr;62(4):679–686. doi: 10.1161/01.res.62.4.679. [DOI] [PubMed] [Google Scholar]
  13. Ito Y., Miyamori I., Matsubara T., Takeda R., Higashida H. Cromakalim, a vasodilator, differentially inhibits Ca2+ currents in NG108-15 neuroblastoma x glioma hybrid cells. FEBS Lett. 1990 Mar 26;262(2):313–316. doi: 10.1016/0014-5793(90)80217-7. [DOI] [PubMed] [Google Scholar]
  14. Kajioka S., Kitamura K., Kuriyama H. Guanosine diphosphate activates an adenosine 5'-triphosphate-sensitive K+ channel in the rabbit portal vein. J Physiol. 1991 Dec;444:397–418. doi: 10.1113/jphysiol.1991.sp018885. [DOI] [PMC free article] [PubMed] [Google Scholar]
  15. McPherson G. A., Angus J. A. Phentolamine and structurally related compounds selectively antagonize the vascular actions of the K+ channel opener, cromromakalim. Br J Pharmacol. 1989 Jul;97(3):941–949. doi: 10.1111/j.1476-5381.1989.tb12035.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  16. Osterrieder W. Modification of K+ conductance of heart cell membrane by BRL 34915. Naunyn Schmiedebergs Arch Pharmacol. 1988 Jan;337(1):93–97. doi: 10.1007/BF00169483. [DOI] [PubMed] [Google Scholar]
  17. Plant T. D., Henquin J. C. Phentolamine and yohimbine inhibit ATP-sensitive K+ channels in mouse pancreatic beta-cells. Br J Pharmacol. 1990 Sep;101(1):115–120. doi: 10.1111/j.1476-5381.1990.tb12099.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  18. Quast U., Cook N. S. In vitro and in vivo comparison of two K+ channel openers, diazoxide and cromakalim, and their inhibition by glibenclamide. J Pharmacol Exp Ther. 1989 Jul;250(1):261–271. [PubMed] [Google Scholar]
  19. Sanguinetti M. C., Scott A. L., Zingaro G. J., Siegl P. K. BRL 34915 (cromakalim) activates ATP-sensitive K+ current in cardiac muscle. Proc Natl Acad Sci U S A. 1988 Nov;85(21):8360–8364. doi: 10.1073/pnas.85.21.8360. [DOI] [PMC free article] [PubMed] [Google Scholar]
  20. 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]
  21. Spuler A., Lehmann-Horn F., Grafe P. Cromakalim (BRL 34915) restores in vitro the membrane potential of depolarized human skeletal muscle fibres. Naunyn Schmiedebergs Arch Pharmacol. 1989 Mar;339(3):327–331. doi: 10.1007/BF00173587. [DOI] [PubMed] [Google Scholar]
  22. 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]
  23. 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]
  24. Trube G., Rorsman P., Ohno-Shosaku T. Opposite effects of tolbutamide and diazoxide on the ATP-dependent K+ channel in mouse pancreatic beta-cells. Pflugers Arch. 1986 Nov;407(5):493–499. doi: 10.1007/BF00657506. [DOI] [PubMed] [Google Scholar]
  25. Weik R., Neumcke B. Effects of potassium channel openers on single potassium channels in mouse skeletal muscle. Naunyn Schmiedebergs Arch Pharmacol. 1990 Sep;342(3):258–263. doi: 10.1007/BF00169435. [DOI] [PubMed] [Google Scholar]

Articles from British Journal of Pharmacology are provided here courtesy of The British Pharmacological Society

RESOURCES