Phenformin has a direct inhibitory effect on the ATP-sensitive potassium channel

European Journal of Pharmacology

Volumn 634, Issue 1-3, 2010, Pages 26-32

  Aziz, Qadeer ^a   Thomas, Alison ^a   Khambra, Tapsi ^a   Tinker, Andrew ^a  

^a UNIVERSITY COLLEGE LONDON   (United Kingdom)

Author keywords

AMPK; KATP channel; Phenformin; Vascular smooth muscle cell; Whole cell patch clamp

Indexed keywords

ADENOSINE TRIPHOSPHATE SENSITIVE POTASSIUM CHANNEL; ADENYLATE KINASE; GLIBENCLAMIDE; INWARDLY RECTIFYING POTASSIUM CHANNEL SUBUNIT KIR6.1; INWARDLY RECTIFYING POTASSIUM CHANNEL SUBUNIT KIR6.2; LEMAKALIM; METFORMIN; N (1 ADAMANTYL) N' CYCLOHEXYL 4 MORPHOLINECARBOXAMIDINE; PHENFORMIN; POTASSIUM CHANNEL BLOCKING AGENT;

ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DOSE RESPONSE; DRUG PROTEIN BINDING; DRUG STRUCTURE; ENZYME ACTIVATION; ENZYME INHIBITION; FEMALE; HEART MUSCLE CELL; HUMAN; HUMAN CELL; IC 50; MALE; MOUSE; NONHUMAN; PANCREAS ISLET BETA CELL; PATCH CLAMP; PRIORITY JOURNAL; PROTEIN EXPRESSION; SMOOTH MUSCLE FIBER; VASCULAR SMOOTH MUSCLE; ACTION POTENTIAL; ANIMAL; ANTAGONISTS AND INHIBITORS; C57BL MOUSE; CELL LINE; COMPARATIVE STUDY; DRUG EFFECTS; PHYSIOLOGY;

ACTION POTENTIALS; ANIMALS; CELL LINE; DOSE-RESPONSE RELATIONSHIP, DRUG; FEMALE; HUMANS; KATP CHANNELS; MALE; MICE; MICE, INBRED C57BL; PHENFORMIN; POTASSIUM CHANNEL BLOCKERS;

EID: 77951208745     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejphar.2010.02.023     Document Type: Article

References (39)

1. Aguilar-Bryan L., Nichols C.G., Wechsler S.W., Clement J.P., Boyd A.E., Gonzalez G., Herrera-Sosa H., Nguy K., Bryan J., Nelson D.A. Cloning of the beta cell high-affinity sulfonylurea receptor: a regulator of insulin secretion. Science 1995, 268:423-426.
2. + channel channel/enzyme multimer: metabolic gating in the heart. J. Mol. Cell. Cardiol. 2005, 38:895-905.
3. Babenko A.P., Aguilar-Bryan L., Bryan J. A view of sur/KIR6.X, KATP channels. Annu. Rev. Physiol. 1998, 60:667-687.
4. Beech D.J., Zhang H., Nakao K., Bolton T.B. K channel activation by nucleotide diphosphates and its inhibition by glibenclamide in vascular smooth muscle cells. Br. J. Pharmacol. 1993, 110:573-582.
5. Bergheim I., Guo L., Davis M.A., Lambert J.C., Beier J.I., Duveau I., Luyendyk J.P., Roth R.A., Arteel G.E. Metformin prevents alcohol-induced liver injury in the mouse: critical role of plasminogen activator inhibitor-1. Gastroenterology 2006, 130:2099-2112.
6. Cui Y., Giblin J.P., Clapp L.H., Tinker A. A mechanism for ATP-sensitive potassium channel diversity: functional coassembly of two pore-forming subunits. Proc. Natl. Acad. Sci. U. S. A. 2001, 98:729-734.
7. Cui Y., Tran S., Tinker A., Clapp L.H. The molecular composition of K(ATP) channels in human pulmonary artery smooth muscle cells and their modulation by growth. Am. J. Respir. Cell Mol. Biol. 2002, 26:135-143.
8. Cui Y., Tinker A., Clapp L.H. Different molecular sites of action for the KATP channel inhibitors, PNU-99963 and PNU-37883A. Br. J. Pharmacol. 2003, 139:122-128.
9. Dell'Aglio D.M., Perino L.J., Kazzi Z., Abramson J., Schwartz M.D., Morgan B.W. Acute metformin overdose: examining serum pH, lactate level, and metformin concentrations in survivors versus nonsurvivors: a systematic review of the literature. Ann. Emerg. Med. 2009, 54:818-823.
10. El Mir M.Y., Nogueira V., Fontaine E., Averet N., Rigoulet M., Leverve X. Dimethylbiguanide inhibits cell respiration via an indirect effect targeted on the respiratory chain complex I. J. Biol. Chem. 2000, 275:223-228.
11. + channels containing Kir6.1 and Kir6.2 subunits. Cardiovasc. Res. 2008, 79:621-631.
12. Giblin J.P., Leaney J.L., Tinker A. The molecular assembly of ATP-sensitive potassium channels. Determinants on the pore forming subunit. J. Biol. Chem. 1999, 274:22652-22659.
13. + channel currents expressed in Xenopus oocytes: a reinterpretation. J. Physiol. 1997, 504(Pt 1):35-45.
14. Hallows K.R., Kobinger G.P., Wilson J.M., Witters L.A., Foskett J.K. Physiological modulation of CFTR activity by AMP-activated protein kinase in polarized T84 cells. Am. J. Physiol. Cell Physiol. 2003, 284:C1297-C1308.
15. Hardie D.G. The AMP-activated protein kinase pathway-new players upstream and downstream. J. Cell Sci. 2004, 117:5479-5487.
16. Hardie D.G. AMPK: a key regulator of energy balance in the single cell and the whole organism. Int. J. Obes. (Lond.) 2008, 32(Suppl 4):S7-S12.
17. Hardie D.G., Carling D. The AMP-activated protein kinase-fuel gauge of the mammalian cell?. Eur. J. Biochem. 1997, 246:259-273.
18. Hawley S.A., Gadalla A.E., Olsen G.S., Hardie D.G. The antidiabetic drug metformin activates the AMP-activated protein kinase cascade via an adenine nucleotide-independent mechanism. Diabetes 2002, 51:2420-2425.
19. Inagaki N., Gonoi T., Clement J.P., Namba N., Inazawa J., Gonzalez G., Aguilar-Bryan L., Seino S., Bryan J. Reconstitution of IKATP: an inward rectifier subunit plus the sulfonylurea receptor. Science 1995, 270:1166-1170.
20. + channel. J. Biol. Chem. 1996, 271:24321-24324.
21. Kovalev H., Quayle J.M., Kamishima T., Lodwick D. Molecular analysis of the subtype-selective inhibition of cloned KATP channels by PNU-37883A. Br. J. Pharmacol. 2004, 141:867-873.
22. Miki T., Suzuki M., Shibasaki T., Uemura H., Sato T., Yamaguchi K., Koseki H., Iwanaga T., Nakaya H., Seino S. Mouse model of Prinzmetal angina by disruption of the inward rectifier Kir6.1. Nat. Med. 2002, 8:466-472.
23. Muzyamba M., Farzaneh T., Behe P., Thomas A., Christesen H.B., Brusgaard K., Hussain K., Tinker A. Complex ABCC8 DNA variations in congenital hyperinsulinism: lessons from functional studies. Clin. Endocrinol. (Oxf.) 2007, 67:115-124.
24. Owen M.R., Doran E., Halestrap A.P. Evidence that metformin exerts its anti-diabetic effects through inhibition of complex 1 of the mitochondrial respiratory chain. Biochem. J. 2000, 348(Pt 3):607-614.
25. + channels?. Circ. Res. 2003, 93:646-655.
26. Rodrigo G.C., Standen N.B. ATP-sensitive potassium channels. Curr. Pharm. Des. 2005, 11:1915-1940.
27. Saeedi R., Parsons H.L., Wambolt R.B., Paulson K., Sharma V., Dyck J.R., Brownsey R.W., Allard M.F. Metabolic actions of metformin in the heart can occur by AMPK-independent mechanisms. Am. J. Physiol. Heart Circ. Physiol. 2008, 294:H2497-H2506.
28. Saito T., Yoshida S. Effects of biguanides on short-circuit current in frog skin. Am. J. Physiol. 1984, 247:F277-F281.
29. Schafer G. On the mechanism of action of hypoglycemia-producing biguanides. A reevaluation and a molecular theory. Biochem. Pharmacol. 1976, 25:2005-2014.
30. Schulz M., Schmoldt A. Therapeutic and toxic blood concentrations of more than 800 drugs and other xenobiotics. Pharmazie 2003, 58:447-474.
31. Seino S. ATP-sensitive potassium channels: a model of heteromultimeric potassium channel/receptor assemblies. Annu. Rev. Physiol. 1999, 61:337-362.
32. + channels. J. Cell. Physiol. 2007, 210:224-236.
33. Teramoto N. Pharmacological profile of U-37883A, a channel blocker of smooth muscle-type ATP-sensitive K channels. Cardiovasc. Drug Rev. 2006, 24:25-32.
34. + channel. Curr. Opin. Neurobiol. 1998, 8:316-320.
35. + channels in the absence of the sulphonylurea receptor. Nature 1997, 387:179-183.
36. + transport across H441 lung cells. J. Physiol. 2005, 566:781-792.
37. + channel. J. Physiol. 1997, 499(Pt 3):715-720.
38. Zhang L., He H., Balschi J.A. Metformin and phenformin activate AMP-activated protein kinase in the heart by increasing cytosolic AMP concentration. Am. J. Physiol. Heart Circ. Physiol. 2007, 293:H457-H466.
39. Zhou G., Myers R., Li Y., Chen Y., Shen X., Fenyk-Melody J., Wu M., Ventre J., Doebber T., Fujii N., Musi N., Hirshman M.F., Goodyear L.J., Moller D.E. Role of AMP-activated protein kinase in mechanism of metformin action. J. Clin. Invest. 2001, 108:1167-1174.