Hansen, J.B., Arkhammar, P.O., Bodvarsdottir, T.B. et al. Inhibition of insulin secretion as a new drug target in the treatment of metabolic disorders. Curr Med Chem 2004, 11: 1595-615.
Zimmet, P., Alberti K.G., Shaw, J. Global and societal implications of the diabetes epidemic. Nature 2001, 414: 782-7.
Turner, R.C. The UK. Prospective diabetes study. A review. Diabetes Care 1998, 21(Suppl. 3): C35-8.
Viviane, E.M. Type 2 diabetes in children and adolescents: The next epidemic? Curr Med Res Opin 2006, 22: 297-306.
Bandyopadhyay, P. Advances in the understanding of diabetes mellitus. Drug News Perspect 2004, 17: 477-87.
Gianani, R., Eisenbarth, G. The stages of type1A diabetes: 2005. Immunol Rev 2005, 204: 232-49.
Daneman, D. Type 1 diabetes. Lancet 2006, 367: 847-58.
Seissler, J., Scherbaum, W.A. Autoimmune diagnostics in diabetes mellitus. Clin Chem Lab Med 2006, 44: 133-7.
Faideau, B., Larger, E., Lepault, F. et al. Role of β-cells in type 1 diabetes pathogenesis. Diabetes 2005, 54(Suppl. 2): S87-96.
Jeffery, A. The seeds are sown in childhood-insulin resistance and the global epidemic of type 2 diabetes. In: Focus on Diabetes Mellitus Research. Ford. A.M. (Ed.). Nova Publishers. 2006, 143-69.
Hanefeld, M. Outcome studies in type 2 diabetes. Curr Med Res Opin 2005, 21(Suppl. 1): S41-8.
Chiasson, J.L., Rabasa-Lhoret, R. Prevention of type 2 diabetes. Insulin resistance and β-cell function. Diabetes 2004, 53(Suppl. 3): S34-8.
Sjoeholm, A., Nystroem, T. Inflammation and etiology of type 2 diabetes. Diabetes Metab Res Rev 2006, 22: 4-10.
Leahy, J. Pathogenesis of type 2 diabetes mellitus. Arch Med Res 2005, 36: 197-209.
Maedler, K., Spinas, G., Lehmann, R. et al. Glucose induces β-cell apoptosis via upregulation of the Fas receptor in human islets. Diabetes 2001, 50: 1683-90.
Bjorklund, A., Lansner, A., Grill, V. Glucose-induced [Ca 2+], abnormalities in human pancreatic islets: Important role of overstimulation. Diabetes 2000, 49: 1840-8.
Poitout, V., Robertson, R. Minireview: Secondary β-cell failure in type 2 diabetes: A convergence of glucotoxicity and lipotoxicity. Endocrinology 2002, 143: 339-42.
Chan, C. Beta-cell stimulus-secretion coupling defects in rodent models of obesity. Can J Physiol Pharmacol 1995, 73: 1414-24.
Koulouridis, E. Insulin and human obesity. Pediatr Endocrinol Rev 2004, 1(Suppl. 3): 438-42.
Beloff-Chain, A. Hyperinsulmemia and obesity. In: Recent Advances in Obesity Research. 1987, 240-5.
Sempoux, C., Guiot, Y., Lefevre, A. et al. Neonatal hyperinsulinemic hypoglycemia: Heterogeneity of the syndrome and keys for differential diagnosis. J Clin Endocrinol Metab 1998, 83: 1455-61.
Dunne, M., Cosgrove, K., Shepherd, R. et al. Hyperinsulinism in infancy: From basic science to clinical disease. Physiol Rev 2004, 84: 239-75.
Verkarre, V., Fournet, J., de Lonlay, P. et al. Paternal mutation of the sulfonylurea receptor (SUR1) gene and material loss of 11p15 imprinted genes lead to persistent hyperinsulinism in focal adenomatous hyperplasia. J Clin Invest 1998, 102: 1286-91.
Dunne, M., Kane, C., Shepherd, R. et al. Familial persistent hyperinsulinemic hypoglycaemia of infancy and mutations in the sulfonylurea receptor. New Engl J Med 1997, 336: 703-6
Aynsley-Green, A., Hussain, K., Hall, J. et al. The practical management of hyperinsulinism in infancy. Arch Dis Child 2000, 82: F98-107.
Ruutiainen, K., Seppala, M. Polycystic ovary syndrome: Evolution of a concept. Curr Opin Obstet Gynecol 1991, 3: 326-35.
Goodarzi, M., Azziz, R. Diagnosis, epidemiology, and genetics of the polycystic ovary syndrome. Best Pract Res Clin Endocrinol Metab 2006, 20: 193-205.
Legro, R. Diabetes prevalence and risk factors in polycystic ovary syndrome. Curr Opin Endocrinol Diabetes 2002, 9: 451-8
Baillargeon, J.P., Nestler, J. Polycystic ovary syndrome: A syndrome of ovarian hypersensitivity to insulin? J Clin Endocrinol Metab 2006, 91: 22-4.
Frerichs, H., Creutzfeldt, W. Hypoglycemia. I. Insulin secreting tumors. Clin Endocrinol Metab 1976, 5: 747-67.
Flatt, P. Defective regulation of insulin secretion in diabetes and insulinoma. Biochem Soc Trans 1990, 18: 124-7.
Vassilopoulou-Sellin, R., Ajani, J. Islet cell tumors of the pancreas. Endocrinol Metab Clin N Am 1994, 23: 53-65.
Efrat, S. Regulation of insulin secretion: Insights from engineered β-cell lines. Ann NY Acad Sci 2004, 1014: 88-96.
Petersen, O., Dunne, M. Regulation of K+ channels plays a crucial role in the control of insulin secretion. Pflügers Arch 1989, 414: S115-20.
Lebrun, P., Antoine, M.H., Herchuelz, A. Minireview: K+ channel openers and insulin release. Life Sci 1992, 51: 795-806.
Aguilar-Bryan, L., Bryan, J., Nakazaki, M. Of mice and men: K ATP channels and insulin secretion. Rec Prog Horm Res 2001, 56: 47-68.
Thorens, B. GLUT2 in pancreatic and extra-pancreatic gluco-detection. Mol Membrane Biol 2001, 18: 265-73.
Nichols, C., Shyng, S., Nestorowicz, A. et al. Adenosine diphosphate as an intracellular regulator of insulin secretion. Science 1996, 272: 1785-7.
Cosgrove, K., Shepherd, R., Fernandez, E. et al. Causes and therapy of hyperinsulinism in infancy. Curr Opin Endocrinol Diabetes 2004, 11: 31-8.
Kane, C., Lindley, K., Johnson, P. et al. Therapy for persistent hyperinsulinemic hypoglycemia of infancy. Understanding the responsiveness of β cells to diazoxide and somatostatin. J Clin Invest 1997, 100(7): 1888-93.
Goode, P., Farndon, J., Anderson, J. et al. Diazoxide in the management of patients with insulinoma. World J Surg 1986, 10: 586-92.
Gill, G., Rauf, O., MacFarlane, I. Diazoxide treatment for insulinoma: A national UK survey. Postgrad Med J 1997, 73: 640-1.
Krassas, G., Kaltsas, T., Pontikides, N. et al. Leptin levels in women with polycystic ovary syndrome before and after treatment with diazoxide. Eur J Endocrinol 1998, 139: 184-9.
Welt, C., Taylor, A., Martin, K. et al. Serum inhibin B in polycystic ovary syndrome: Regulation by insulin and luteinizing hormone. J Clin Endocrinol Metab 2002, 87: 5559-65.
Best, J., Judzewitsch, R., Pfeifer, M. et al. The effect of chronic sulfonylurea therapy on hepatic glucose production in non-insulino-dependent diabetes. Diabetes 1982, 31: 333-8.
Groop, L. Sulfonylureas in NIDDM. Diabetes Care 1992, 15: 737-54.
Rendell, M. The role of sulfonylureas in the management of type 2 diabetes mellitus. Drugs 2004, 64: 1339-58.
Björk, E., Berne, C., Kämpe, O. et al. Diazoxide treatment at onset preserves residual insulin secretion in adults with autoimmune diabetes. Diabetes 1996, 45: 1427-30.
Bjork, E., Berne, C., Karlsson, F. Induction of β-cell rest in type 1 diabetes. Studies on the effects of octreotide and diazoxide. Diabetes Care 1998, 21: 427-30.
Rasmussen, S., Sorensen, T., Hansen, J.B. et al. Functional rest through intensive treatment with insulin and potassium channel openers preserves residual β-cells function and mass in acutely diabetic BB rats. Horm Metab Res 2000, 32: 294-300.
Ritzel, R., Hansen, J.B., Veldhuis, J. et al. Induction of β-cell rest by a Kir6.2/SUR1-selective K(ATP)-channel opener preserves β-cell insulin stores and insulin secretion in human islets cultured at high (11 mM) glucose. J Clin Endocrinol Metab 2004, 89: 795-805.
Bjork, E., Kampe, O., Andersson, A. et al. Glucose regulation of the autoantigen GAD65 in human pancreatic islets. J Clin Endocrinol Metab 1992, 75: 1574-6.
Leahy, J., Bumbalo, L., Chen, C. Diazoxide causes recovery of β-cell glucose responsiveness in 90% pancreatectomized diabetic rats. Diabetes 1994, 43: 173-9.
Alemzadeh, R., Slonim, A., Zdanowicz, M. et al. Modification of insulin resistance by diazoxide in obese Zucker rats. Endocrinology 1993, 133: 705-12.
Aizawa, T., Taguchi, N., Nahoko, S. et al. Prophylaxis of genetically determined diabetes by diazoxide: A study in a rat model of naturally occurring obese diabetes. J Pharmacol Exp Ther 1995, 275: 194-9.
Alemzadeh, R., Tushaus, K. Modulation of adipoinsular axis in prediabetic Zucker diabetic fatty rats by diazoxide. Endocrinology 2004, 145: 5476-84.
Surwit, R., Dixon, T., Petro, A. et al. Diazoxide restores β3-adrenergic receptor function in diet-induced obesity and diabetes. Endocrinology 2000, 141: 3630-7.
Bjorklund, A., Bondo Hansen, J., Falkmer, S. et al. Openers of ATP-dependent K+-channels protect against a signal-transduction linked and not freely reversible defect of insulin secretion in a rat islet transplantation model of type 2 diabetes. Diabetologia 2004, 47: 885-91.
Carr, R., Brand, C., Bodvarsdottir, T. et al. NN414, a SUR1/Kir6.2-selective potassium channel opener, reduces blood glucose and improves glucose tolerance in the VDF Zucker rat. Diabetes 2003, 52: 2513-8.
Alemzadeh, R., Fledelius, C., Bodvarsdottir, T. et al. Attenuation of hyperinsulinemia by NN414, a SUR1/KiR6.2 selective K+-adenosine triphosphate channel opener, improves glucose tolerance and lipid profile in obese Zucker rats. Metabolism 2004, 53: 441-7.
Alemzadeh, R., Jacobs, W., Pitukcheewanont, P. Antiobesity effect of diazoxide in obese Zucker rats. Metabolism 1996, 45: 334-41.
Alemzadeh, R., Langley, G., Upchurch, L. et al. Beneficial effect of diazoxide in obese hyperinsulinemic adults. J Endocrinol Metab 1998, 83: 1911-5.
Pocai, A., Lam, T., Tony, K. et al. Hypothalamic KATP channels control hepatic glucose production. Nature 2005, 434: 1026-31.
Pocai, A., Obici, S., Schwartz, G. et al. A brain-liver circuit regulates glucose homeostasis. Cell Metab 2005, 1: 53-61.
Evans, M., McCrimmon, R., Flanagan, D. et al. Hypothalamic ATP-sensitive K+ channels play a key role in sensing hypoglycemia and triggering counterregulatory epinephrine and glucagon responses. Diabetes 2004, 53: 2542-51.
Seino, S., Miki, T. Physiological and physiopathological roles of ATP-sensitive K+ channels. Prog Biophys Mol Biol 2003, 81: 133-76.
Kolb, H.A. Potassium channels in excitable and non-excitable cells. Rev Physiol Biochem Pharmacol 1990, 15: 51-79.
Seino, S. ATP-sensitive potassium channels: A model of heteromultimeric potassium channel/receptor assemblies. Annu Rev Physiol 1999, 61: 337-62.
Aguilar-Bryan, L., Nichols, C., Wechsler, S. et al. Cloning of the β cell high-affinity sulfonylurea receptor: A regulator of insulin secretion. Science 1995, 268: 423-6.
Inagaki, N., Gonio, T., Clement, J.P. Reconstitution of I KATP: An inward rectifier subunit plus a sulfonylurea receptor. Science 1995, 270: 1166-70.
Clement, J.P., Kunjilwar, K., Gonzalez, G. et al. Association and stoichiometry of KATP channel subunits. Neuron 1997, 18: 827-38.
Shyng, S., Nichols, C. Octameric stoichiometry of the KATP channel complex. J Gen Physiol 1197, 110: 655-64.
Moreau, C., Prost, A.L., Derand, R. et al. SUR, ABC proteins targeted by KATP channel openers. J Mol Cell Cardiol 2005, 38: 951-63.
Bryan, J., Crane, A., Vila-Carriles, W.H. et al. Insulin secret-agogues, sulfonylurea receptors and KATP channels. Curr Pharm Des 2005, 11: 2699-716.
Tabachnick, I., Gulbenkian, A., Yannell, A. The hyperglycemic activity of benzothiadiazine and other diuretics. Life Sci 1965, 4: 1931-6.
Rubin, A., Roth, F., Winbury, M. et al. New class of antihypertensive agents. Science 1961, 133: 2067.
Black, J. Diazoxide and the treatment of hypoglycemic: An historical review. Ann NY Acad Sci 1968, 150: 194-203.
Wales, J., Krees, S., Grant, A. et al. Structure-activity relationships of benzothiadiazine compounds as hyperglycemic agents. J Pharmacol Exp Ther 1968, 164: 421-32.
Trube, G., Rorsman, P., Ohno-Shosaku, T. Opposite effects of tolbutamide and diazoxide on the ATP-dependent K+ channel in mouse pancreatic β-cells. Pflugers Arch 1986, 407: 493-9.
Kumar, G., Dastoor, F., Robayo, J. et al. Side effects of diazoxide. JAMA - J Am Med Assoc 1976, 235: 275-6.
de Tullio, P., Pirotte, B., Lebrun, P. et al. 3- And 4-substituted 4H-pyhdo[4,3-e]-1,2,4-thiadiazine 1,1-dioxides as potassium channel openers: Synthesis, pharmacological evaluation and structure-activity relationships. J Med Chem 1996, 39: 937-48.
Wollweber, H., Horstmann, H., Stoepel, K. et al. 3-(Amino)-2H-1,2,4- benzothiadiazine-1,1-dioxide mit antihypertensiver und potentieller diabetogen Wirkung. Arzneim-Forsch 1981, 31: 279-88.
Pirotte, B., de Tullio, P., Lebrun, P. et al. 3-(Alkylamino)-4H- pyrido[4,3-e]-1.2,4-thiadiazine 1,1-dioxides as powerful inhibitors of insulin release from rat pancreatic β-cells: A new class of potassium channel openers? J Med Chem 1993, 36: 3211-3.
Lebrun, P., Antoine, M.H., Ouedraogo, R. et al. Pyridothiadiazines as potent inhibitors of glucose-induced insulin release. Adv Exp Med Biol 1997, 426: 145-8.
Pirotte, B. Antoine, M.H., de Tullio, P. et al. A pyridothiadiazine (BPDZ 44) as a new and potent activator of ATP-sensitive K+ channels. Biochem Pharmacol 1994, 47: 1381-6.
Antoine, M.H., Pirotte B., Hermann, M. et al. Cationic and secretory effects of BPDZ 44 and diazoxide in rat pancreatic islets. Experientia 1994, 50: 830-2
Lebrun, P., Antoine, M.H., Ouedraogo, R. et al. Activation of ATP-dependent K+ channels and inhibition of insulin release: Effect of BPDZ 62. J Pharmacol Exp Ther 1996, 277: 156-62.
Pirotte, B., Ouedraogo, R., de Tullio, P et al. 3-Alkylamino-4H- pyrido[2,3-e]-1,2,4-thiadiazine 1,1-dioxides structurally related to diazoxide and pinacidil as potassium channel openers acting on vascular smooth muscle cells: Design, synthesis, and pharmacological evaluation. J Med Chem 2000, 43: 1456-66.
de Tullio, P., Becker, B., Boverie, S. et al. Toward tissue-selective pancreatic β-cells KATP channel openers belonging to 3-alkylamino-7-halo-4H-1,2,4-benzothiadiazine 1,1-dioxides. J Med Chem 2003, 46: 3342-53.
Boverie, S., Antoine, M-H., Somers, F. et al. Effect on K ATP channel activation properties and tissue selectivity of the nature of the substituent in the 7- and the 3-position of 4H-1,2,4- benzothiadiazine 1,1-dioxides. J Med Chem 2005, 48: 3492-503.
de Tullio, P., Boverie, S., Becker, B. et al. 3-Alkylamino-4H-1,2,4- benzothiadiazine 1,1-dioxides as ATP-sensitive potassium channel openers: Effect of 6,7-disubstitution on potency and tissue selectivity. J Med Chem 2005, 48: 4990-5000.
Lebrun, P., Arkhammar, P., Antoine, M.-H. et al. A potent diazoxide analogue activating ATP-sensitive K+ channels and inhibiting insulin release. Diabetologia 2000, 43: 723-32.
de Tullio, P., Dupont, L., Francotte, P. et al. 3D-Quantitative structure-activity relationships of KATP channel openers belonging to the 3-alkylamino-4H-1,2,4-benzo and 3-alkylamino-4H-1,2.4-pyhdothiadiazine 1,1-dioxide families. J Med Chem 2006, In press.
Cosgrove, K., Antoine, M.-H., Lee, A. et al. BPDZ 154 activates adenosine 5+-triphosphate-sensitive potassium channels: In vitro studies using rodent insulin-secreting cells and islets isolated from patients with hyperinsulinism. J Clin Endocrinol Metab 2002, 87: 4860-8.
Dabrowski, M., Ashcroft, P.M., Ashfield, R. et al. The novel diazoxide analog 3-isopropylamino-7-methoxy-4H-1,2,4-benzothiadiazine 1,1-dioxide is a selective Kir6.2/SUR1 channel opener. Diabetes 2002, 51: 1896-906.
Peat, A., Townsend, C., Worley, J.F. et al. Synthesis and evaluation of 7-substituted-3-cyclobutylamino-4H-1,2,4-benzothiadiazine-1,1-dioxide derivatives as KATP channel agonists. Bioorg Med Chem Lett 2002, 12: 2977-80.
Nielsen, F., Bodvarsdottir, T., Worsaae, A. et al. 6-Chloro-3- alkylamino-4H-thieno[3,2-e]-1,2,4-benzothiadiazine 1,1-dioxide derivatives potently and selectively activate ATP-sensitive potassium channels of pancreatic β-cells. J Med Chem 2002, 45: 4171-87.
Dabrowski, M., Larsen, T., Ashcroft, F. et al. Potent and selective activation of the pancreatic β-cell type KATP channel by two novel diazoxide analogues. Diabetologia 2003, 46: 1375-82
Nielsen, F., Ebdrup, S., Jensen, A. et al. New 3-alkylamino-4H-thieno- 1,2,4-thiadiazine 1,1-dioxides derivatives activate ATP-sensitive potassium channels of pancreatic β cells. J Med Chem 2006, 49: 4127-39.
Kullin, M., Li, Z., Hansen, J.B. et al. K(ATP) channel openers protect rat islets against the toxic effect of streptozotocin. Diabetes 2000, 49: 1131-6.
Kullin, M., Li, Z., Hansen, J.B. et al. Protection of rat pancreatic islets by potassium channel openers against alloxan, sodium nitroprusside and interleukin-1β mediated suppression: Possible involvement of the mitochondrial membrane potential. Diabetologia 2003, 46: 80-8.
Skak, K., Gotfredsen, C., Lundsgaard, D. et al. Improved β-cell survival and reduced insulitis in a type 1 diabetic rat model after treatment with a β-cell-selective KATP channel opener. Diabetes 2004, 53: 1089-95.
Zdravkovic, M., Kruse, M., Rost, K. et al. The effects of NN414, a SUR1/Kir6.2 selective potassium channel opener, in healthy male subjects. J Clin Pharmacol 2005, 45: 763-72.
Pirotte, B., de Tullio, P., Antoine, M.-H. et al. New insights into the development of ATP-sensitive potassium channel openers. Expert Opin Ther Patents 2005, 15: 497-504.
Schou, S., Hansen, H., Tagmose, T. et al. Synthesis and pharmacological evaluation of 4H-1,4-benzothiazine-2-carbonitrile 1,1-dioxide and N-(2-cyanomethylsulfonylphenyl) acylamide derivatives as potential activators of ATP-sensitive potassium channels. Bioorg Med Chem 2005, 13: 141-55.
Lebrun, P., Devreux, V., Hermann, M. et al. Pinacidil inhibits insulin release by increasing K+ outflow from pancreatic β-cells. Eur J Pharmacol 1988, 156: 283-6.
Tagmose, T., Mogensen, J., Agerholm, P. et al. Phenylcyanoguanidines as inhibitors of glucose-induced insulin secretion from β cells. Bioorg Med Chem Lett 2001, 11: 1749-52.
Tagmose, T., Schou, S., Mogensen, J. et al. Arylcyanoguanidines as activators of Kir6.2/SUR1KATP channels and inhibitors of insulin release. J Med Chem 2004, 47: 3202-11.
Tagmose, T., Zaragoza, F., Boonen, H. et al. Synthesis and biological activity of 3,3-diamino-sulfonylacrylonitriles as novel inhibitors of glucose-induced insulin secretion from β cells. Bioorg Med Chem 2003, 11: 931-40.
Sebille, S., de Tullio, P., Boverie, S. et al. Recent developments in the chemistry of potassium channel activators: The cromakalim analogs. Curr Med Chem 2004, 11: 1213-22.
Mannhold, R. Structure-activity relationships of KATP channel openers. Curr Top Med Chem 2006, 6: 1031-47.
Cosgrove, K., Straub, S., Barnes, P. et al. Y-26763: ATP-sensitive K+ channel activation and the inhibition of insulin release from human pancreatic β-cells. Eur J Pharmacol 2004, 486: 133-9.
Sebille, S., de Tullio, P. Becker, B. et al. 4,6-Disubsituted 2,2-dimethylchromans structurally related to the KATP channel opener cromakalim: Design, synthesis, and effect on insulin release and vascular tone. J Med Chem 2005, 48: 614-21.
Sebille, S., Gall, D., de Tullio, P. et al. Design, synthesis, and pharmacological evaluation of R/S-3,4-dihydro-2,2-dimethyl-6-halo-4- (phenylaminocarbonylamino)-2H-1-benzopyrans: Toward tissue-selective pancreatic β-cell KATP channel openers structurally related to (±)-cromakalim. J Med Chem 2006, 49: 4690-7.
Nielsen, F., Jacobsen, P., Worsaae, A. et al. 2-(4-Methoxyphenoxy)-5- nitro-N-(4-sulfamoylphenyl)benzamide activates Kir6.2/SUR1 KATP channels. Bioorg Med Chem Lett 2004, 14: 5727-30.
Peat, A., Townsend, C., McKay, C. et al. 3-Trifluoromethyl-4-nitro-5- arylpyrazoles are novel KATP channel agonists. Bioorg Med Chem Lett 2004, 14: 813-6.
