A potent diazoxide analogue activating ATP-sensitive K+ channels and inhibiting insulin release

Diabetologia

Volumn 43, Issue 6, 2000, Pages 723-732

  Lebrun, P ^a   Arkhammar, P ^b   Antoine, M H ^a   Nguyen, Q A ^a   Hansen, J Bondo ^b   Pirotte, B ^c  

^a UNIVERSITÉ LIBRE DE BRUXELLES   (Belgium)

^b NOVO NORDISK A S   (Denmark)

^c UNIVERSITY OF LIÈGE   (Belgium)

Author keywords

ATP sensitive K+ channel; Diazoxide; Insulin release; Rat pancreatic islets

Indexed keywords

73 (7 CHLORO 3 ISOPROPYLAMINO 4H 1,2,4 BENZOTHIADIAZINE 1,1 DIOXIDE); DIAZOXIDE DERIVATIVE; GLUCOSE; HYPERGLYCEMIC AGENT; INSULIN; POTASSIUM CHANNEL; UNCLASSIFIED DRUG;

ARTICLE; CALCIUM TRANSPORT; DRUG MECHANISM; DRUG POTENCY; GLUCAGON BLOOD LEVEL; INSULIN RELEASE; PRIORITY JOURNAL; VASODILATATION;

EID: 0034124168     PISSN: 0012186X     EISSN: None     Source Type: Journal    
DOI: 10.1007/s001250051370     Document Type: Article

References (32)

1. 1. Koch-Weser J (1976) Diazoxide. N Engl J Med 294: 1271-1274
2. 2. Meissner T, Brune W, Mayatepek E (1997) Persistent hyperinsulinaemic hypoglycaemia of infancy: therapy, clinical outcome and mutational analysis. Eur J Pediatr 156: 754-757
3. 3. Vlahos WD, Seemayer TA, Yale JF (1991) Diabetes prevention in BB rats by inhibition of endogenous insulin secretion. Metabolism 40: 825-829
4. 4. Alemzadeh R, Slonim AE, Zdanowicz ML, Maturo J (1993) Modification of insulin resistance by diazoxide in obese Zucker rats. Endocrinology 133: 705-712
5. 5. Aizawa T, Taguchi N, Sato Y et al. (1995) Prophylaxis of genetically determined diabetes by diazoxide: a study in a rat model of naturally occuring obese diabetes. J Pharmacol Exp Ther 275: 194-199
6. 6. Greenwood RH, Mahler RF, Hales CN (1976) Improvement in insulin secretion in diabetes after diazoxide. Lancet 28: 444-447
7. 7. Björk E, Berne C, Kämpe O, Wibell L, Oskarsson P, Karlsson FA (1996) Diazoxide treatment at onset preserves residual insulin secretion in adults with autoimmune diabetes. Diabetes 45: 1427-1430
8. 8. Alemzadeh R, Langley G, Upchurch L, Smith P, Slonim AE (1998) Beneficial effect of diazoxide in obese hyperinsulinemic adults. J Clin Endocrinol Metab 83: 1911-1915
9. ATP channels. Annu Rev Physiol 60: 667-687
10. 10. Ashcroft FM, Rorsman P (1989) Electrophysiology of the pancreatic B-cell. Prog Biophys Mol Biol 54: 87-143
11. + channel openers and insulin release. Life Sci 51: 795-806
12. + channels. Trends Neurosci 21: 288-294
13. 13. Leclercq-Meyer V, Marchand J, Woussen-Colle MC, Giroix MH, Malaisse WJ (1985) Multiple effects of leucine on glucagon, insulin and somatostatin secretion from the perifused rat pancreas. Endocrinology 116: 1168-1174
14. 2+ influx into pancreatic B cell. Am J Physiol 242: E59-E66
15. 15. Lebrun P, Malaisse WJ, Herchuelz A (1982b) Nutrient-induced intracellular calcium movement in rat pancreatic B cell. Am J Physiol 243: E196-E205
16. 16. Lebrun P, Devreux V, Hermann M, Herchuelz A (1989) Similarities between the effects of pinacidil and diazoxide on ionic and secretory events in rat pancreatic islets. J Pharmacol Exp Ther 250: 1011-1018
17. + channels and inhibition of insulin release: effect of BPDZ 62. J Pharmacol Exp Ther 277: 156-162
18. + fluxes in isolated islets. Pflügers Arch 373: 237-242
19. 19. Efrat S, Linde S, Kofod H et al. (1988) Beta-cell lines derived from transgenic mice expressing a hybrid insulin gene-oncogene. Proc Natl Acad Sci USA 85: 9037-9041
20. 4(3)) in model systems and cells. Chem Phys Lipids 69: 137-150
21. 21. Antoine MH, Berkenboom G, Fang ZY, Fontaine J, Herchuelz A, Lebrun P (1992) Mechanical and ionic response of rat aorta to diazoxide. Eur J Pharmacol 216: 299-306
22. 22. de Tullio P, Pirotte B, Lebrun et al. (1996) 3-and 4-substituted 4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxides as potassium channel openers: synthesis, pharmacological evaluation, and structure-activity relationships. J Med Chem 39: 937-948
23. 23. Pirotte B, de Tullio P, Lebrun P et al. (1993) 3-(Alkylamino)-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxides as powerful inhibitors of insulin release from rat pancreatic B-cells: a new class of potassium channel openers? J Med Chem 36: 3211-3213
24. 24. Di Bella M, Rinaldi M, Fabio U, Manicardi G (1973) Azione antimicrobica di derivati dell' 1,2,4-benzotiadiazin-1,1-diossido. Farmaco 28: 411-417
25. 25. Raffa L, Di Bella M, Ferrari P, Rinaldi M (1974) Azione cardiovascolare di derivati dell' 1,2,4-benzothiadiazin-1,1-diossido. Farmaco 29: 411-423
26. 26. Lebrun P, Atwater I (1985) Effects of the calcium channel agonist, BAY K 8644, on electrical activity in mouse pancreatic B-cells. Biophys J 48: 919-930
27. 27. Girard Y, Atkinson JG, Rokach J (1979) A new synthesis of 1, 2, 4-benzothiadiazines and a selective preparation of o-aminobenzenesulphonamides. J Chem Soc [Perkin 1]: 1043-1047
28. 28. Godfraind T, Miller R, Wibo M (1986) Calcium antagonism and calcium entry blockade. Pharmacol Rev 38: 321-416
29. + permeability and membrane potential in insulin secreting cells. In: Flatt PR (ed) Nutrient regulation of insulin secretion. Portland Press, London, pp 173-191
30. 30. Malaisse WJ, Lebrun P (1990) Mechanisms of sulfonylurea-induced insulin release. Diabetes Care 13[Suppl 3]:9-17
31. 2+ inflow into rat pancreatic islets. Am J Physiol 258: E529-E533
32. ATP channels. Eur J Pharmacol 313: 229-235