PAR-1622 is a selective peroxisome proliferator-activated receptor γ partial activator with preserved antidiabetic efficacy and broader safety profile for fluid retention

Archives of Pharmacal Research

Volumn 32, Issue 5, 2009, Pages 721-727

  Kim, Mi Kyung ^a   Chae, Yu Na ^a   Kim, Hae Sun ^a   Choi, Song Hyen ^a   Son, Moon Ho ^a   Kim, Soon Hoe ^a   Kim, Jin Kwan ^a   Moon, Ho Sang ^a   Park, Sang Kuk ^a   Shin, Young Ah ^b   Kim, Jae Gyu ^b   Lee, Chun Ho ^b   Lim, Joong In ^a   Shin, Chang Yell ^a  

^a Dong A Research Center   (South Korea)

^b Yuhan Research Institute   (South Korea)

Author keywords

Insulin resistance; PAR 1622; Partial activator; Peroxisome proliferator activated receptor; Plasma volume

Indexed keywords

[2 ETHOXY 3 [4 [5 [4 [5 (METHOXYMETHYL)ISOXAZOL 3 YL]PHENYL] 3 METHYLTHIOPHEN 2 YL]METHOXY]PHENYL]PROPANOIC ACID; EVANS BLUE; INT 131; PAR 1622; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR ALPHA; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR DELTA; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA AGONIST; ROSIGLITAZONE; UNCLASSIFIED DRUG; (S) 2 ETHOXY 3 (4 (5 (4 (5 (METHOXYMETHYL)ISOXAZOL 3 YL)PHENYL) 3 METHYLTHIOPHEN 2 YL)METHOXYPHENYL)PROPANOIC ACID; (S)-2-ETHOXY-3-(4-(5-(4-(5-(METHOXYMETHYL)ISOXAZOL-3-YL)PHENYL)-3-METHYLTHIOPHEN-2-YL)METHOXYPHENYL)PROPANOIC ACID; 2,4 THIAZOLIDINEDIONE DERIVATIVE; ANTIDIABETIC AGENT; ISOXAZOLE DERIVATIVE; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA; PROPIONIC ACID DERIVATIVE; THIOPHENE DERIVATIVE;

ADIPOCYTE; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CELL DIFFERENTIATION; CONTROLLED STUDY; DRUG ACTIVITY; DRUG EFFICACY; DRUG RECEPTOR BINDING; DRUG SAFETY; FLUID RETENTION; HEMODILUTION; HUMAN; HUMAN CELL; HYPERGLYCEMIA; INSULIN RESISTANCE; MALE; MESENCHYMAL STEM CELL; MOUSE; NONHUMAN; PLASMA VOLUME; ADIPOGENESIS; ANIMAL; BLOOD VOLUME; CELL CULTURE; COMPARATIVE STUDY; DISEASE MODEL; DOSE RESPONSE; DRUG EFFECT; DRUG POTENTIATION; ELECTROLYTE BALANCE; GENETIC TRANSFECTION; GENETICS; GLUCOSE BLOOD LEVEL; INSTITUTE FOR CANCER RESEARCH MOUSE; METABOLISM; NON INSULIN DEPENDENT DIABETES MELLITUS; ORAL DRUG ADMINISTRATION; PARTIAL AGONISM; REPORTER GENE;

ADIPOGENESIS; ADMINISTRATION, ORAL; ANIMALS; BLOOD GLUCOSE; BLOOD VOLUME; CELLS, CULTURED; DIABETES MELLITUS, TYPE 2; DISEASE MODELS, ANIMAL; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG PARTIAL AGONISM; GENES, REPORTER; HUMANS; HYPOGLYCEMIC AGENTS; ISOXAZOLES; MALE; MESENCHYMAL STEM CELLS; MICE; MICE, INBRED ICR; PPAR GAMMA; PROPIONIC ACIDS; THIAZOLIDINEDIONES; THIOPHENES; TRANSFECTION; WATER-ELECTROLYTE BALANCE;

EID: 67649366027     PISSN: 02536269     EISSN: 19763786     Source Type: Journal    
DOI: 10.1007/s12272-009-1511-8     Document Type: Article

References (23)

1. J. J. Acton III R. M. Black A. B. Jones D. E. Moller L. Colwell T. W. Doebber K. L. Macnaul J. Berger H. B. Wood 2005 Benzoyl 2-methyl indoles as selective PPARgamma modulators Bioorg. Med. Chem. Lett. 15 357 362
2. T. Allen F. Zhang S. A. Moodie L. E. Clemens A. Smith F. Gregoire A. Bell G. E. Muscat T. A. Gustafson 2006 Halofenate is a selective peroxisome proliferator-activated receptor gamma modulator with antidiabetic activity Diabetes. 55 2523 2533
3. M. Bajaj S. Suraamornkul L. J. Hardies L. Glass N. Musi R. A. DeFronzo 2007 Effects of peroxisome proliferatoractivated receptor (PPAR)-alpha and PPAR-gamma agonists on glucose and lipid metabolism in patients with type 2 diabetes mellitus Diabetologia. 50 1723 1731
4. L. Chen B. Yang J. A. McNulty L. G. Clifton J. G. Binz A. M. Grimes J. C. Strum W. W. Harrington Z. Chen T. W. Balon S. A. Stimpson K. K. Brown 2005 GI262570, a peroxisome proliferator-activated receptor {gamma} agonist, changes electrolytes and water reabsorption from the distal nephron in rats J. Pharmacol. Exp. Ther. 312 718 725
5. Y. J. Hung S. H. Lin D. Pei S. W. Kuo C. H. Hsieh C. T. He C. Hsing Lee S. C. Fan W. H. Sheu 2006 Rosiglitazone improves insulin sensitivity in nonobese subjects with impaired glucose tolerance: the role of adiponectin and C-reactive protein Metabolism. 55 439 444
6. K. Iwasaki R. Zhang M. A. Perhonen J. H. Zuckerman B. D. Levine 2004 Reduced baroreflex control of heart period after bed rest is normalized by acute plasma volume restoration Am J. Physiol. Regul. Integr. Comp. Physiol. 287 R1256 1262
7. C. Knouff J. Auwerx 2004 Peroxisome proliferatoractivated receptor-gamma calls for activation in moderation: lessons from genetics and pharmacology Endocr. Rev. 25 899 918
8. Li, Y., Wang, Z., Motani, A., McGee, L. R., Learned, M., Timmermans, P. B., and Chen, J. L., T0903131 (T131): A selective modulator of PPARgamma. 64th Annu. Meet Sci. Sess. Am. Diabetes Assoc., Abst 659-P (2004).
9. K. Liu R. M. Black J. J. Acton III R. Mosley S. Debenham R. Abola M. Yang R. Tschirret-Guth L. Colwell C. Liu M. Wu C. F. Wang K. L. MacNaul M. E. McCann D. E. Moller J. P. Berger P. T. Meinke A. B. Jones H. B. Wood 2005 Selective PPARgamma modulators with improved pharmacological profiles Bioorg. Med. Chem. Lett. 15 2437 2440
10. D. C. Merrill A. W. Cowley Jr. 1987 Chronic effects of vasopressin on fluid volume distribution in conscious dogs Am. J. Physiol. 252 F26 31
11. P. Misra R. Chakrabarti R. K. Vikramadithyan G. Bolusu S. Juluri J. Hiriyan C. Gershome A. Rajjak P. Kashireddy S. Yu S. Surapureddi C. Qi Y. J. Zhu M. S. Rao J. K. Reddy R. Ramanujam 2003 PAT5A: a partial agonist of peroxisome proliferator-activated receptor gamma is a potent antidiabetic thiazolidinedione yet weakly adipogenic J. Pharmacol. Exp. Ther. 306 763 771
12. S. Mittra G. Sangle R. Tandon S. Sharma S. Roy V. Khanna A. Gupta J. Sattigeri L. Sharma P. Priyadarsiny S. K. Khattar R. S. Bora K. S. Saini V. S. Bansal 2007 Increase in weight induced by muraglitazar, a dual PPARalpha/gamma agonist, in db/db mice: adipogenesis/or oedema? Br. J. Pharmacol. 150 480 487
13. R. W. Nesto D. Bell R. O. Bonow V. Fonseca S. M. Grundy E. S. Horton M. Le Winter D. Porte C. F. Semenkovich S. Smith L. H. Young R. Kahn 2003 Thiazolidinedione use, fluid retention, and congestive heart failure: a consensus statement from the American Heart Association and American Diabetes Association. October 7, 2003 Circulation. 108 2941 2948
14. S. E. Nissen K. Wolski E. J. Topol 2005 Effect of muraglitazar on death and major adverse cardiovascular events in patients with type 2 diabetes mellitus JAMA. 294 2581 2586
15. J. M. Olefsky 2000 Treatment of insulin resistance with peroxisome proliferator-activated receptor gamma agonists J. Clin. Invest. 106 467 472
16. D. Porte Jr. M. W. Schwartz 1996 Diabetes complications: why is glucose potentially toxic? Science. 272 699 700
17. S. M. Rangwala M. A. Lazar 2004 Peroxisome proliferatoractivated receptor gamma in diabetes and metabolism Trends Pharmacol. Sci. 25 331 336
18. R. S. Rosenson J. D. Otvos D. S. Freedman 2002 Relations of lipoprotein subclass levels and low-density lipoprotein size to progression of coronary artery disease in the Pravastatin Limitation of Atherosclerosis in the Coronary Arteries (PLAC-I) trial Am. J. Cardiol. 90 89 94
19. S. H. Tannehill-Gregg T. P. Sanderson D. Minnema R. Voelker B. Ulland S. M. Cohen L. L. Arnold B. E. Schilling C. R. Waites M. A. Dominick 2007 Rodent carcinogenicity profile of the antidiabetic dual PPAR alpha and gamma agonist muraglitazar Toxicol. Sci. 98 258 270
20. P. Tontonoz E. Hu R. A. Graves A. I. Budavari B. M. Spiegelman 1994 mPPAR gamma 2: tissue-specific regulator of an adipocyte enhancer Genes Dev. 8 1224 1234
21. H. E. Xu M. H. Lambert V. G. Montana K. D. Plunket L. B. Moore J. L. Collins J. A. Oplinger S. A. Kliewer R. T. Gampe Jr. D. D. McKee J. T. Moore T. M. Willson 2001 Structural determinants of ligand binding selectivity between the peroxisome proliferator-activated receptors Proc. Natl. Acad. Sci. U. S. A. 98 13919 13924
22. H. Zhang A. Zhang D. E. Kohan R. D. Nelson F. J. Gonzalez T. Yang 2005 Collecting duct-specific deletion of peroxisome proliferator-activated receptor gamma blocks thiazolidinedione-induced fluid retention Proc. Natl. Acad. Sci. U. S. A. 102 9406 9411
23. Y. L. Zhulun Z. Wang A. Motani L. R. Mcgee M. Learned P. B. Timmermans J. L. Chen 2004 T0903131 (T131); A selective modulator of PPARγ Diabetes 53 Suppl2 A157