Hypoglycaemic and insulinotropic effects of a novel oral antidiabetic agent, (-)-N-(trans-4-isopropylcyclohexane- carbonyl)-D-phenylalanine (A-4166)

British Journal of Pharmacology

Volumn 120, Issue 1, 1997, Pages 137-145

  Ikenoue, Takao ^a   Akiyoshi, Megumi ^a   Fujitani, Shoji ^a   Okazaki, Kyoko ^a   Kondo, Nobuo ^a   Maki, Toshio ^a  

^a AJINOMOTO CO INC   (Japan)

Author keywords

A 4166; Insulin secretion; Islets of langerhans; Sulphonylurea

Indexed keywords

GLIBENCLAMIDE; GLICLAZIDE; GLUCOSE; INSULIN; NATEGLINIDE; ORAL ANTIDIABETIC AGENT; SULFONYLUREA; TOLBUTAMIDE;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CONCENTRATION RESPONSE; CONTROLLED STUDY; DOG; DOSE TIME EFFECT RELATION; DRUG ABSORPTION; DRUG BINDING; DRUG CLEARANCE; DRUG POTENCY; GLUCOSE BLOOD LEVEL; HUMAN; HUMAN CELL; INSULIN BLOOD LEVEL; INSULIN LIKE ACTIVITY; INSULIN RELEASE; MALE; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; ORAL DRUG ADMINISTRATION; PANCREAS ISLET; PRIORITY JOURNAL; RAT;

ANIMALS; BINDING, COMPETITIVE; BLOOD GLUCOSE; CALCIUM; CELL LINE; CYCLOHEXANES; DIAZOXIDE; DIURETICS; DOGS; GLYBURIDE; HYPOGLYCEMIC AGENTS; INSULIN; ISLETS OF LANGERHANS; MALE; PHENYLALANINE; RATS; RATS, WISTAR; SODIUM CHLORIDE SYMPORTER INHIBITORS; STIMULATION, CHEMICAL;

EID: 0031038234     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0700875     Document Type: Article

References (38)

1. AKIYOSHI, M , FUJITANI, S., IKENOUE, T., OKAZAKI, K., KONDO, N., MAKI, T. & KIKUCHI, M. (1994). Possible therapy for postprandial hyperglycemia with strict glycemic control by a newly developed hypoglycemic agent, A-4166 15th International Diabetes Federation Congress (Abstract) 419.
2. AKIYOSHI, M., KAKEI, M., NAKAZAKI, M. & TANAKA, H. (1995). A newly hypoglycemic agent, A-4166, inhibits ATP-sensitive potassium channels in rat pancreatic β-cells. Am. J. Physiol., 268, E185-E193.
3. ASPLUND, K., WIHOLM, B.E. & LITHNER, F. (1983). Glibenclamide-associated hypoglycaemia: a report on 57 cases. Diabetologia, 24, 412-417.
4. BECK-NIELSEN, H., HOTHER-NIELSEN, O. & PEDERSEN, O. (1988). Mechanism of action of sulphonylureas with special reference to the extrapancreatic effect: An overview. Diabetic Med. 5, 613-620.
5. 50) of an enzymatic reaction. Biochem. Pharmacol., 22, 3099-3108.
6. DAVALLI, A.M., PONTIROLI, A.E., SOCCI, C., BERTUZZI, F., FATTOR, B., BRAGHI, S., CARLO, V.D. & POZZA, G. (1992). Human islets chronically exposed in vitro to different stimuli become unresponsive to the same stimuli given acutely: evidence supporting specific desensitization rather than β-cell exhaustion. J. Clin. Endocrinol. Melab., 74, 790-794.
7. FERNER, R.E. & NEIL, H.A.W. (1988). Sulphonylureas and hypoglycaemia. Br. Med. J., 296, 949-950.
8. FILIPPONI, P., MARCELLI, M., NICOLETTI, I., PACIFICI, R., SANTEUSANIO, F. & BRUNETTI, P. (1983). Suppressive effect of long term sulphonylurea treatment on A, B, and D cells of normal rat pancreas. Endocrinology, 113, 1972-1979.
9. FUJITANI, S., IKENOUE, T., AKIYOSHI, M., MAKI, T. & YADA, T. (1996). Somatostatin and insulin secretion due to common mechanisms by a new hypoglycemic agent, A-4166, in perfused rat pancreas. Metabolism, 45, 184-189.
10. 2+ influx. Endocrinology, 134, 1395-1400.
11. GRECO, A.V., CAPUTO, S., BERTOLI, A. & GHIRLANDA, G. (1992). The beta cell function in NIDDM patients with secondary failure. Horm. Metab. Res., 24, 280-283.
12. GROOP, L.C., PELKONEN, R., KOSKIMIES, S., BOTTAZZO, G.F. & DONIACH, D. (1986). Secondary failure to treatment with oral antidiabetic agents in non-insulin-dependent diabetes. Diabetes Care, 9, 129-133.
13. GROOP, L.C., RATHEISER, K., LUZI, L., MELANDER, A., SIMONSON, D.C., PETRIDES, A., BONADONNA, R.C., WIDEN, E. & DEFRONZO, R.A. (1991). Effect of sulphonylurea on glucose-stimulated insulin secretion in healthy and non-insulin dependent diabetic subjects: a dose-response study. Acta. Diabetol., 28, 162-168.
14. GROOP, L., SCHALIN, C., KALLUNKI, A.F., WIDEN, E., EKSTRAND, A. & ERIKSSON, J. (1989). Characteristics of non-insulin dependent diabetic patients with secondary failure to oral antidiabetic therapy. Am. J. Med., 87, 183-190.
15. 2+ indicators with greatly improved fluorescence properties. J. Biol. Chem., 260, 3440-3450.
16. HENQUIN, J.C. (1990). Established, unsuspected and novel pharmacological insulin secretagogues. In New Antidiabetic Drugs., ed. Bailey, C.J. & Flatt, P.R. pp. 93-106. London: Smith-Gordon and Co.
17. JOOST, H.G. (1985). Extrapancreatic effects of hypoglycemic sulfonylureas: still a controversial issue. Trends Pharmacol. Sci., 6, 239-241.
18. KIKUCHI, M., KUZUYA, T., AKANUMA, Y., KOSAKA, K. & AY4166 STUDY GROUP. (1994). Early Phase II Study of a novel oral hypoglycemic agent, AY4166. I5th International Diabetes Federation Congress (Abstract) 418.
19. KOSAKA, K., KUZUYA, T. & HAGURA, R. (1994). Insulin secretory response in Japanese type 2 (non-insulin-dependent) diabetic patients. Diabetes Res. Clin. Pract., 24, (Suppl.), S101-S110.
20. LEBOVITZ, H.E. (1984). Cellular loci of sulfonylurea actions. Diabetes Care, 7, (Suppl. 1), 67-71.
21. LEBOVITZ, H.E. (1992). Oral antidiabetic agents. Drugs, 44, (Suppl. 3), 21-28.
22. LECLERCQ-MEYER, V. AKKAN, A.G., MARCHAND, J. & MALAISSE, W.J. (1991). Effects of glimepiride and glibenclamide on insulin and glucagon secretion by the perfused rat pancreas. Biochem. Pharmacol., 42, 1634-1637.
23. LUZI, L. & DEFRONZO, R.A. (1989). Effect of loss of first-phase insulin secretion on hepatic glucose production and tissue glucose disposal in humans. Am. J. Physiol., 257, E241-E246.
24. MALAISSE, W.J., GARCIA-MORALES, P., DUFRANE, S.P., SENER, A. & VALVERDE, I. (1984). Forskolin-induced activation of adenylate cyclase, cyclic adenosine monophosphate production and insulin release in rat pancreatic islets. Endocrinology, 115, 2015-2020.
25. OHKUBO, Y., KISHIKAWA, H., ARAKI, E., MIYATA, T., ISAMI, S., MOTOYOSHI, S., KOJIMA, Y., FURUYOSHI, N. & SHICHIRI, M. (1995). Intensive insulin therapy prevents the progression of diabetic microvascular complications in Japanese patients with non-insulin-dependent diabetes mellitus: a randomized prospective 6-year study. Diabetes Res. Clin. Pract., 28, 103-117.
26. PANTEN, U., SCHWANSTECHER, M. & SCHWANSTECHER, C. (1996). Sulfonylurea receptors and mechanisms of sulfonylurea action. Exp. Clin. Endocrinol., 104, 1-9.
27. POLONSKY, K.S., GIVEN, B.D., HIRSCH, L.J., TILLIL, H., SHAPIRO, E.T., BEEBE, C., FRANK, B.H., GALLOWAY, J.A. & CAUTER, E.V. (1988). Abnormal patterns of insulin secretion in non-insulin-dependent diabetes mellitus. N. Engl. J. Med., 318, 1231-1239.
28. PORTE, D. (1991). β-Cells in type II diabetes mellitus. Diabetes, 40, 166-180.
29. SAKO, Y., WASADA, T., UMEDA, F. & IBAYASHI, H. (1986). Effect of glibenclamide on pancreatic hormone release from isolated perifused islets of normal and cysteamine-treated rats. Metabolism, 35, 944-949.
30. SELTZER, H.S. (1989). Drug-induced hypoglycemia. Endocrinol. Metab. Clin. North. Am., 18, 163-183.
31. SHAPIRO, E.T., CAUTER, E.V., TILLIL, H., GIVEN, B.D., HIRSCH, L., BEEBE, C., RUBENSTEIN, A.H. & POLONSKY, K.S. (1989). Glyburide enhances the responsiveness of the β-cell to glucose but does not correct the abnormal patterns of insulin secretion in noninsulin-dependent diabetes mellitus. J. Clin. Endocrinol. Metab., 69, 571-576.
32. SHINKAI, H., NISHIKAWA, M., SATO, Y., TOI, K., KUMASHIRO, I., SETO, Y., FUKUMA, M., DAN, K. & TOYOSHIMA, S. (1989). N-(cyclohexylcarbonyl)-D-phenylalanines and related compounds. A new class of oral hypoglycemic agents. J. Med. Chem., 32, 1436-1441.
33. SHINKAI, H., TOI, K., KUMASHIRO, I., SETO, Y., FUKUMA, M., DAN, K. & TOYOSHIMA, S. (1988). N-Acylphenylalanines and related compounds. A new class of oral hypoglycemic agents. J. Med. Chem., 31, 2092-2097.
34. SIMA, A.A.F. & CHAKRABARTI, S. (1992). Long-term suppression of postprandial hyperglycaemia with acarbose retards the development of neuropathies in the BB/W-rat. Diabetologia, 35, 325-330.
35. THE DCCT RESEARCH GROUP (1993). The effect of intensive treatment of diabetes on the development and progression of long-term complications in insulin-dependent diabetes mellitus. N. Engl. J. Med., 329, 977-986.
36. + channel in mouse pancreatic β-cells. Pflügers Arch., 407, 493-499.
37. YADA, T. & FUJITANI, S. (1994). Pancreatic beta-cells under metabolic inhibition are activated by A-4166, a novel hypoglycemic agent, more effectively than by tolbutamide. 15th International Diabetes Federation Congress (Abstract), 293.
38. YADA, T., SAKURADA, M., IHIDA, K., NAKATA, M., MURATA, F., ARIMURA, A. & KIKUCHI, M. (1994). Pituitary adenylate cyclase activating polypeptide is an extraordinarily potent intrapancreatic regulator of insulin secretion from islet β-cells. J. Biol. Chem., 269, 1290-1293.