The insulinotropic mechanism of the novel hypoglycaemic agent JTT-608: Direct enhancement of Ca2+ efficacy and increase of Ca2+ influx by phosphodiesterase inhibition

British Journal of Pharmacology

Volumn 129, Issue 5, 2000, Pages 901-908

  Mukai, Eri ^a   Ishida, Hitoshi ^a,b   Fujimoto, Shimpei ^a   Kajikawa, Mariko ^a   Okamoto, Yoshimasa ^a   Fujita, Jun ^a   Hamamoto, Yoshiyuki ^a   Tsuura, Yoshiyuki ^a   Yamada, Yuichiro ^a   Furukawa, Noboru ^c   Ohta, Takeshi ^c   Seino, Yutaka ^a  

^a KYOTO UNIVERSITY   (Japan)

^b KYORIN UNIVERSITY SCHOOL OF MEDICINE   (Japan)

^c JAPAN TOBACCO INC   (Japan)

Author keywords

Cyclic AMP; Insulin secretion; JTT 608; Pancreatic islets; Phosphodiesterase inhibitor

Indexed keywords

4 (4 METHYLCYCLOHEXYL) 4 OXOBUTYRIC ACID; ANTIDIABETIC AGENT; CALCIUM ION; CYCLIC AMP; DIAZOXIDE; FORSKOLIN; GLUCOSE; INSULIN; ISOBUTYLMETHYLXANTHINE; NITRENDIPINE; PHOSPHODIESTERASE; PHOSPHODIESTERASE INHIBITOR; POTASSIUM ION; UNCLASSIFIED DRUG;

ANIMAL TISSUE; ARTICLE; CALCIUM TRANSPORT; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG POTENTIATION; INSULIN LIKE ACTIVITY; INSULIN RELEASE; MALE; NONHUMAN; PANCREAS ISLET; PRIORITY JOURNAL; RAT;

EID: 0034052124     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0703133     Document Type: Article

References (32)

1. Ämmälä, C., Ashcroft, F.M. & Rorsman, P. (1993). Calcium-independent potentiation of insulin release by cyclic AMP in single β-cells. Nature, 363, 356-358.
2. Ashcroft, F.M & Rorsman, P. (1989). Properties and functions of ATP-sensitive K-channel. Prog. Biophys. Molec. Biol., 54, 87-143.
3. Beavo, J.A. (1995). Cyclic nucleotide phosphodiesterases: functional implication of multiple isoforms. Physiol. Rev., 75, 725-748.
4. ATP current in intact mouse pancreatic B-cells. Biochem. Biophys. Res. Commun., 207, 33-39.
5. Ding, W.-G. & Gromada, J. (1997). Protein kinase A-dependent stimulation of exocytosis in mouse pancreatic β-cells by glucose-dependent insulinotropic polypeptide. Diabetes, 46, 615-621.
6. 2+ sensitivity in β-cells. Endocrinology, 139, 1133-1140.
7. + channels in mouse β-cells. J. Clin. Invest., 89, 1288-1295.
8. 2+ oscillations in isolated pancreatic β-cells. J. Biol. Chem., 266, 12207-12210.
9. Gromada, J., Bokvist, K., Ding, W.-G., Holst, J.J., Nielsen, J.H. & Rorsman, P. (1998). Glucagon-like peptide 1(7-36) amide stimulates exocytosis in human pancreatic β-cells by both proximal and distal regulatory steps in stimulus-secretion coupling. Diabetes, 47, 57-65.
10. Jones, P.M., Fyles, J.M. & Howell, S. (1986). Regulation of insulin secretion by cAMP in rat islets of Langerhans permcabilised by high-voltage discharge. FEBS Letters, 205, 205-209.
11. 2+ channel activities in pancreatic β cells of non-insulin-dependent diabetes mellitus GK rats. J. Clin. Invest., 97, 2417-2425.
12. Leibowttz, M.D., Biswas, C., Brady, E.J., Conti, M., Cullinan, C.A., Hayes, N.S., Manganiello, V.C., Saperstein, R., Wang, L., Zafian, P.T. & Berger, J. (1995). A novel insulin secretagogue is a phosphodiesterase inhibitor. Diabetes, 44, 67-74.
13. Lu, M., Wheeler, M.B., Leng, X.-H. & Boyd, III, A.E. (1993). The role of the free cytosolic calcium level in β-cell signal transduction by gastric inhibitory polypeptide and glucagon-like peptide I (7-37). Endocrinology. 132, 94-100.
14. Manganiello, V.C., Murata, T., Taira, M., Belfrage, P. & Degerman, E. (1995). Diversity in cyclic nucleotide phosphodiesterase isoenzyme families. Arch. Biochem. Biophys., 322, 1-13.
15. Ohta, T., Furukawa, N., Komuro, G., Yonemori, F. & Wakitani, K. (1999a). JTT-608 restores impaired early insulin secretion in diabetic Goto-Kakizaki rats. Br. J. Pharmacol., 126, 1674-1680.
16. Ohta, T., Furukawa, N., Yonemori, F. & Wakitani, K. (1999b). JTT-608 controls blood glucose by enhancement of glucose-stimulated insulin secretion in normal and diabetes mellitus rats. Eur. J. Pharmacol., 367, 91-99.
17. Okamoto, Y., Ishida, H., Tsuura, Y., Yasuda, K., Matsubara, H., Nishimura, M., Mizuno, N., Ikeda, H. & Seino, Y. (1995). Hyperresponse in calcium-induced insulin release from electrically permeabilized pancreatic islets of diabetic GK rats and its defective augmentation by glucose. Diabetologia. 38, 772-778.
18. Parker, J.C., Vanvolkenburg, M.A., Ketchum, R.J., Brayman, K.L. & Andrews, K.M. (1995). Cyclic phosphodiesterases of human and rat islets of Langerhans: contribution of types III and IV to the modulation of insulin secretion. Biochem. Biophys. Res. Commun., 217, 916-923.
19. 2+ influx in rat pancreatic β-cell. Diabetes, 41, 438-443.
20. Shafiee-Nick, R., Pyne, N.J. & Furman, B.L. (1995). Effects of type-selective phosphodiesterase inhibitors on glucose-induced insulin secretion and islet phosphodiesterase activity. Br. J. Pharmacol., 115, 1486-1492.
21. Sharp, G.W.G. (1979). The adenylate cyclase-cyclic AMP system in islets of Langerhans and its role in the control of insulin release. Diabetologia, 16, 287-296.
22. Shinkai, H., Ozeki, H., Motomura, T., Ohta, T., Furukawa, N. & Uchida, T. (1998). 4-(trans-4-methylcyclohexyl)-4-oxobutyric acid (JTT-608). A new class of antidiabetic agent. J. Med. Chem., 41, 5420-5428.
23. Siegel, E.G., Wollheim, C.B., Kikuchi, M., Renold, A.E & Sharp, G.W.G. (1980). Dependency of cyclic AMP-induced insulin release on intra-and extracellular calcium in rat islets of Langerhans. J. Clin. Invest., 65, 233-241.
24. Sutton, R., Peters, M., McShane, P., Gray, D.W.R. & Morris, P.J. (1986). Isolation of rat pancreatic islets by ductal injection of collagenase. Transplantation, 42, 689-691.
25. 2+ by forskolin and phorbol ester. FEBS Letters, 183, 430-432.
26. Thompson, W.J. & Appleman, M.M. (1971). Multiple cyclic nucleotide phosphodiesterase activities from rat brain. Biochem J., 10, 311-316.
27. Tsuji, K., Taminato, T., Usami, M., Ishida, H., Kitano, N., Fukumoto, H., Koh, G., Kurose, T., Yamada, Y., Yano, H., Seino, Y. & Imura, H. (1988). Characteristic features of insulin secretion in the streptozotocin-induced NIDDM rat model. Metabolism. 37, 1040-1044.
28. Ward, W.K., Beard, J.C., Halter, J.B., Pfeiffer, M.A. & Porte, D. (1984). Pathophysiology of insulin secretion in non-insulin dependent diabetes mellitus. Diabetes Care, 7, 491-502.
29. 2+ channel activity. Endocrinology, 133, 1685-1692.
30. 2+ in rat pancreatic β-cells. Diabetes, 45, 295-301.
31. Zhao, A.Z., Bornfeld, K.E. & Beavo, J.A. (1998). Leptin inhibits insulin secretion by activation of phosphodiesterase 3B. J. Clin. Invest., 102, 869-873.
32. Zhao, A.Z., Zhao, H., Teague, J., Fujimoto, W. & Beavo, J.A. (1997). Attenuation of insulin secretion by insulin-like growth factor 1 is mediated through activation of phosphodiesterase 3B. Proc. Natl. Acad. Sci. U.S.A., 94, 3223-3228.