Stimulation of glucose-dependent insulin secretion by a potent, selective sst 3 antagonist

ACS Medicinal Chemistry Letters

Volumn 3, Issue 4, 2012, Pages 289-293

  Pasternak, Alexander ^a   Feng, Zhe ^a   De Jesus, Reynalda ^a   Ye, Zhixiong ^a   He, Shuwen ^a   Dobbelaar, Peter ^a   Bradley, Scott A ^a   Chicchi, Gary G ^a   Tsao, Kwei Lan ^a   Trusca, Dorina ^a   Eiermann, George J ^a   Li, Cai ^a   Feng, Yue ^a   Wu, Margaret ^a   Shao, Qing ^a   Zhang, Bei B ^a   Nargund, Ravi ^a   Mills, Sander G ^a   Howard, Andrew D ^a   Yang, Lihu ^a   Zhou, Yun Ping ^a   more..

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

glucose stimulated insulin secretion; somatostatin; sst 3; type 2 diabetes

Indexed keywords

3 (5 PHENYL 1H IMIDAZOL 2 YL) 1 (TETRAHYDRO 2H PYRAN 4 YL) 2,3,4,9 TETRAHYDRO 1H BETA CARBOLINE; ANTIDIABETIC AGENT; BETA CARBOLINE DERIVATIVE; GLUCOSE; HORMONE RECEPTOR BLOCKING AGENT; INSULIN; SOMATOSTATIN RECEPTOR 3 ANTAGONIST; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DRUG CLEARANCE; DRUG ELIMINATION; DRUG HALF LIFE; DRUG MECHANISM; DRUG POTENCY; DRUG RECEPTOR BINDING; GLUCOSE TOLERANCE TEST; IC 50; INSULIN RELEASE; INTRAPERITONEAL GLUCOSE TOLERANCE TEST; MAXIMUM PLASMA CONCENTRATION; MOUSE; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; ORAL GLUCOSE TOLERANCE TEST; PANCREAS ISLET BETA CELL; PRIORITY JOURNAL; WILD TYPE;

MUS;

EID: 84859739676     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/ml200272z     Document Type: Article

References (19)

1. Wild, S.; Roglic, G.; Green, A.; Sicree, R.; King, H. Global Prevalence of Diabetes: Estimates for the Year 2000 and Projections for 2030 Diabetes Care 2004, 27, 1047-1053 (Pubitemid 38579764)
2. Zimmet, P; Alberti, K. G. M. M.; Shaw, J. Global and Societal Implications of the Diabetes Epidemic Nature 2001, 414, 782-787 (Pubitemid 34000780)
3. Skyler, J. S. Diabetes Mellitus: Pathogenesis and Treatment Strategies J. Med. Chem. 2004, 47, 4113-4117 (Pubitemid 39045414)
4. Ahren, B. Islet G Protein-coupled Receptors as Potential Targets for Treatment of Type 2 Diabetes Nature Rev. Drug Discovery 2009, 8, 369-385
5. Mohler, M. L.; He, Y.; Wu, Z.; Hwang, D. J.; Miller, D. D. Recent and Emerging Anti-Diabetic targets Med. Res. Rev. 2008, 1-71
6. Weckbecker, G.; Lewis, I.; Albert, R.; Schmid, H. A.; Hoyer, D.; Bruns, C. Opportunities in Somatostatin Research: Biological, Chemical, and Therapeutic Aspects Nature Rev. Drug Discovery 2003, 2, 999-1017 (Pubitemid 37540581)
7. Olias, G; Viollet, C.; Kusserow, H.; Epelbaum, J.; Meyerhof, W. Regulation and Function of Somatostatin Receptors J. Neurochem. 2004, 89 (5) 1057-1091 (Pubitemid 38720193)
8. Florio, T.; Morini, M.; Villa, V.; Arena, S.; Corsaro, A.; Thellung, S.; Culler, M. D.; Pfeffer, V.; Noonan, D. M.; Schettini, G.; Albini, A. Somatostatin Inhibits Tumor Angiogenesis and Growth via Somatostatin receptor-3-mediated Regulation of Endothelial Nitric Oxide Synthase and Mitogen Activated Protein Kinase Activities Endocrinology 2003, 144 (4) 1574-1584 (Pubitemid 36428500)
9. Srikant, C. B. Cell Cycle Dependent Induction of Apoptosis by Somatostatin Analog SMS 201-995 in AtT-20 Mouse Pituitary Cells Biochem. Biophys. Res. Commun. 1995, 209 (2) 400-406
10. Lattuada, D.; Casnici, C.; Venuto, A.; Marelli, O. The Apoptotic Effect of Somatostatin Analog SMS 201-995 on Human Lymphocytes J. Neuroimmunol. 2002, 133 (1-2) 211-216 (Pubitemid 35346744)
11. For a recent review of subtype selective somatostatin receptor ligands, see Wolkenberg, S. E.; Thut, C. J. Recent Progress in the Discovery of Selective Non-Peptide Ligands of Somatostatin Receptors Current Opin. Drug Discovery Dev. 2008, 11 (4) 446-457 (Pubitemid 351950840)
12. 3 Receptor Antagonist [4-(3,4-difluoro-phenyl)-piperazine-1-yl]-{(4 S,4a S,8a R)-2[(S)-3-(6-methoxy- pyridin-3-yl)-2-methyl-propyl]-decahydroisoquinoline-4-yl}-methanone (NVP-ACQ090) Tetrahedron: Asymmetry 2003, 14, 3469-3477 (Pubitemid 37412469)
13. 3 receptor antagonists Bioorg. Med. Chem. Lett. 2010, 20, 1728-1734
14. 3 Selectivity J. Med. Chem. 2001, 44, 2990-3000 (Pubitemid 32879128)
15. Novartis AG (Troxler, T. J.; Hurth, K.; Hoyer, D.) β-Carboline Derivatives and its Pharmaceutical Use Against Depression and Anxiety. U.S. 6,861,430 B2, March 1, 2005.
16. 3 binding assay and the GSIS assay with pancreatic islets, see the Supporting Information and Merck & Co., Inc. (Zhou, Y.-P.; Li, J.; Wu, W.; Shang, J.; Thompson, J. R.; Thornberry, N. A.) Diagnosis and Treatment of Diabetes and Other Disorders. U.S. 2009/0131451A1, May 21, 2009.
17. Wang, J.; Della Penna, K.; Wang, H.; Karczewski, J.; Connolly, T. M.; Koblan, K. S.; Bennett, P. B.; Salata, J. J. Functional and pharmacological properties of canine ERG potassium channels Am. J. Phys. 2003, 284, H256-67
18. Zhou, Y.-P.; Marlen, K.; Palma, J. F.; Schweitzer, A.; Reilly, L.; Gregoire, F. M.; Xu, G. G.; Blume, J. E.; Johnson, J. D. Overexpression of Repressive cAMP Response Element Modulators in High Glucose and Fatty Acid-treated Rat Islets J. Biol. Chem. 2003, 278, 51316-51323
19. For details on the glucose tolerance test models in mice, please see the Supporting Information and Tan, C. P.; Feng, Y.; Zhou, Y.-P.; Eiermann, G. J.; Petrov, A.; Zhou, C.; Lin, S.; Salituro, G.; Meinke, P.; Mosley, R.; Akiyama, T. E.; Einstein, M.; Kumar, S.; Berger, J. P.; Mills, S. G.; Thornberry, N. A.; Yang, L.; Howard, A. D. Selective small-molecule agonists of G protein-coupled receptor 40 promote glucose-dependent insulin secretion and reduce blood glucose in mice Diabetes 2008, 57 (8) 2211-2219