Non-peptidic urotensin-II receptor modulators

Expert Opinion on Therapeutic Patents

Volumn 16, Issue 4, 2006, Pages 467-479

  Jin, Jian ^a   Douglas, Stephen A ^a  

^a GLAXOSMITHKLINE   (United States)

Author keywords

Cardiorenal disease; Metabolic disease; Palosuran (ACT 0586362); SB 706375; Urotensin II (U II); Vasoconstriction

Indexed keywords

2 AMINOQUINOLONE; 4 AMINOQUINOLONE UREA; AC 7954; ACT 058362; ADRENERGIC RECEPTOR; ANGIOTENSIN II; AZEPINE DERIVATIVE; BENZOTHIAZEPINE; CALCIUM ION; CARDIOVASCULAR AGENT; CHOLESTEROL ACYLTRANSFERASE; CISPLATIN; DIHYDROPYRIMIDINONE; DOPAMINE RECEPTOR; ENDOTHELIN 1; KAPPA OPIATE RECEPTOR; MEMBRANE RECEPTOR; MITOGEN ACTIVATED PROTEIN KINASE; NEUROPEPTIDE; ORTHO TRIFLUOROMETHYL ARYLSULFONAMIDE; PALOSURAN; PHENYLEPHRINE; POTASSIUM CHLORIDE; PYRIDINE DERIVATIVE; SB 611812; SB 657510; SB 706375; SEROTONIN RECEPTOR; SOMATOSTATIN RECEPTOR; UNCLASSIFIED DRUG; UNINDEXED DRUG; UROTENSIN II;

ATHEROSCLEROSIS; CARDIOVASCULAR DISEASE; DIABETES MELLITUS; DRUG MECHANISM; DRUG RECEPTOR BINDING; DRUG STRUCTURE; HEART FAILURE; HEART HEMODYNAMICS; HUMAN; HYPERTENSION; IN VITRO STUDY; IN VIVO STUDY; KIDNEY FAILURE; KIDNEY FUNCTION; LIVER CIRRHOSIS; NEPHROTOXICITY; NONHUMAN; PROTEIN FUNCTION; PROTEIN ISOLATION; REVIEW; STRUCTURE ANALYSIS; VASOCONSTRICTION;

EID: 33645753473     PISSN: 13543776     EISSN: None     Source Type: Journal    
DOI: 10.1517/13543776.16.4.467     Document Type: Review

References (62)

1. BERN HA, LEDERIS K: A reference preparation for the study of active substances in the caudal neurosecretory system of teleosts. J. Endocrinol. (1969) 45:xi-xii.
2. BERN HA, PEARSON D, LARSON BA, NISHIOKA RS: Neurohormones from fish tails: the caudal neurosecretory system. I. 'Urophysiology' and the caudal neurosecretory system of fishes. Recent Prog. Horm. Res. (1985) 41:533-552.
3. CONLON JM, O'HARTE F, SMITH DD, TONON MC, VAUDRY H: Isolation and primary structure of urotensin II from the brain of a tetrapod, the frog Rana ridibunda. Biochem. Biophys. Res. Commun. (1992) 188:578-583.
4. COULOUARN Y, JEGOU S, TOSTIVINT H, VAUDRY H, LIHRMANN I: Cloning, sequence analysis and tissue distribution of the mouse and rat urotensin II precursors. FEBS Lett. (1999) 457:28-32.
5. MORI M, SUGO T, ABE M et al.: Urotensin II is the endogenous ligand of a G-protein-coupled orphan receptor, SENR (GPR14). Biochem. Biophys. Res. Commun. (1999) 265:123-129.
6. ELSHOURBAGY NA, DOUGLAS SA, SHABON U et al.: Molecular and pharmacological characterization of genes encoding urotensin-II peptides and their cognate G-protein-coupled receptors from the mouse and monkey. Br. J. Pharmacol. (2002) 136:9-22.
7. AMES RS, SARAU HM, CHAMBERS JK et al.: Human urotensin-II is a potent vasoconstrictor and agonist for the orphan receptor GPR14. Nature (1999) 401:282-286.
8. COULOUARN Y, LIHRMANN I, JEGOU S et al.: Cloning of the cDNA encoding the urotensin II precursor in frog and human reveals intense expression of the urotensin II gene in motoneurons of the spinal cord. Proc. Natl. Acad. Sci. USA (1998) 95:15803-15808.
9. CONLON JM, TOSTIVINT H, VAUDRY H: Somatostatin- and urotensin II-related peptides: molecular diversity and evolutionary perspectives. Regul. Pep. (1997) 69:95-103.
10. ONAN D, HANNAN RD, THOMAS WG: Urotensin II: the old kid in town. Trends Endocrinol. Metab. (2004) 15:175-182.
11. NOTHACKER HP, WANG Z, MCNEIL AM et al.: Identification of the natural ligand of an orphan G-protein-coupled receptor involved in the regulation of vasoconstriction. Nat. Cell. Biol. (1999) 1:383-385.
12. HEROLD CL, DEHM DJ, BUCKLEY PT, FOLEY JJ, DOUGLAS SA: The peptidic somatostatin analogs lanreotide, BIM-23127 and BIM-23042 are urotensin-II receptor ligands. Pharmacologist (2002) 44:170-171.
13. SUGO T, MURAKAMI Y, SHIMOMURA Y et al.: Identification of urotensin II-related peptide as the urotensin II-immunoreactive molecule in the rat brain. Biochem. Biophys. Res. Commun. (2003) 310:860-868.
14. RUSSELL FD: Emerging roles of urotensin-II in cardiovascular disease. Pharmacol. Ther. (2004) 103:223-243.
15. DOUGLAS SA, DHANAK D, JOHNS DG: From 'gills to pills': urotensin-II as a regulator of mammalian cardiorenal function. Trends Pharmacol. Sci. (2004) 25:76-85.
16. CHARLES CJ, RADEMAKER MT, RICHARDS AM, YANDLE TG: Urotensin II: evidence for cardiac, hepatic and renal production. Peptides (2005) 26:2211-2214.
17. ICHIKAWA T, MCMASTER D, LEDERIS K, KOYABASHI H: Isolation and amino acid sequence of urotensin I, a vasoactive and ACTH-releasing neuropeptide, from the carp (Cyprinus carpio) urophysis. Peptides (1982) 3:859-867.
18. HAZON N, BALMENT RJ: Endocrinology In: The Physiology of Fishes. Evans DH (Eds), CRC Press, New York (1998):441-463.
19. LORETZ CA, HOWARD ME, SIEGEL AJ: Ion transport in goby intestine: cellular mechanism of urotensin II stimulation. J. Physiol. (1985) 249:G284-G293.
20. DOUGLAS SA, OHLSTEIN EH: Human urotensin-II, the most potent mammalian vasoconstrictor identified to date, as a therapeutic target for the management of cardiovascular disease. Trends Cardiovasc. Med. (2000) 10:229-237.
21. BEHM DJ, DOE CP, JOHNS DG et al.: Urotensin-II: a novel systemic hypertensive factor in the cat. Naunyn Schmiedeberg's Arch. Pharmacol. (2004) 369:274-280.
22. BÖHM F, PERNOW J: Urotensin II evokes potent vasoconstriction in humans in vivo. Br. J. Pharmacol. (2002) 135:25-27.
23. LIM M, HONISETT S, SPARKES CD, KOMESAROFF P, KOMPA A, KRUM H: Differential effect of urotensin II on vascular tone in normal subjects and patients with chronic heart failure. Circulation (2004) 109:1212-1214.
24. SONDERMEIJER B, KOMPA A, KOMESAROFF P, KRUM H: Effect of exogenous urotensin-II on vascular tone in skin microcirculation of patients with essential hypertension. Am. J. Hypertension (2005) 18:1195-1199.
25. RUSSEL FD, MEYERS D, GALBRAITH AJ et al.: Elevated plasma levels of human urotensin-II immunoreactivity in congestive heart failure. Am. J. Physiol. (2003) 285:H1576-H1581.
26. KOMPA AR, THOMAS WG, SEE F, TZANIDIS A, HANNAN RD, KRUM H: Cardiovascular role of urotensin II: effect of chronic infusion in the rat. Peptides (2004) 25:1783-1788.
27. SONG W, ASHTON N, BALMENT RJ: Effects of single bolus urotensin II injection in anaesthetised rats. J. Physiol. (2003) 552P:P107.
28. WATANABE T, PAKALA R, KATAGIRI T, BENEDICT CR: Synergistic effect of urotensin II with mildly oxidized LDL on DNA synthesis in vascular smooth muscle cells. Circulation (2001) 104:16-18.
29. ZOU Y, NAGAI R, YAMAAKI T: Urotensin II induces hypertrophic responses in cultured cardiomyocytes from neonatal rats. FEBS Lett. (2001) 508:57-60.
30. JOHNS DG, AO Z, NASELSKY D et al.: Urotensin-II-mediated cardiomyocyte hypertrophy: effect of receptor antagonism and role of inflammatory mediators. Naunyn Schmiedeberg Arch. Pharmacol. (2004) 370:238-250.
31. TZANIDIS A, HANNAN RD, THOMAS WG et al.: Direct actions of urotensin II on the heart: implications for cardiac fibrosis and hypertrophy. Circ. Res. (2003) 93:246-253.
32. ONAN D, PIPOLO L, YANG E, HANNAN RD, THOMAS WG: Urotensin II promotes hypertrophy of cardiac myocytes via mitogen-activated protein kinases. Mol. Endocrinol. (2004) 18:2344-2354.
33. MATSUSHITA M, SHICHIRI M, IMAI T et al.: Co-expression of urotensin II and its receptor (GPR14) in human cardiovascular and renal tissues. J. Hypertens. (2001) 19:2185-2190.
34. CHEUNG BM, LEUNG R, MAN YB, WONG LY: Plasma concentration of urotensin II is raised in hypertension. J. Hypertension (2004) 22:1341-1344.
35. DOUGLAS SA, TAYARA L, OHLSTEIN EH, HALAWA N, GIAID A: Congestive heart failure and expression of myocardial urotensin II. Lancet (2002) 359:1990-1997.
36. NG LL, LOKE I, O'BRIEN RJ, SQUIRE IB, DAVIES JE: Plasma urotensin in human systolic heart failure. Circulation (2002) 106:2877-2880.
37. RICHARDS AM, NICHOLLS MG, LAINCHBURY JG, FISHER S, YANDLE TG: Plasma urotensin II in heart failure. Lancet (2002) 360:545-546.
38. LAPP H, BOERRIGTER G, COSTELLO-BOERRIGTER LC et al.: Elevated plasma human urotensin-II-like immunoreactivity in ischemic cardiomyopathy. Int. J. Cardiol. (2004) 94:93-97.
39. BOUSETTE N, PATEL L, DOUGLAS SA, OHLSTEIN EH, GIAID A: Increased expression of urotensin II and its cognate receptor GPR14 in atherosclerotic lesions of the human aorta. Atherosclerosis (2004) 176:117-123.
40. MAGUIRE JJ, KUC RE, WILEY KE, KLEINZ MJ, DAVENPORT AP: Cellular distribution of immunoreactive urotensin-II in human tissues with evidence of increased expression in atherosclerosis and greater constrictor response of small compared to large coronary arteries. Peptides (2004) 25:1767-1774.
41. HASSAN GS, DOUGLAS SA, OHLSTEIN EH, GIAID A: Expression of urotensin-II in human coronary atherosclerosis. Peptides (2005) 26:2464-2472.
42. TOTSUNE K, TAKAHASHI K, ARIHARA Z et al.: Role of urotensin II in patients on dialysis. Lancet (2001) 358:810-811.
43. SHENOUDA A, DOUGLAS SA, OHLSTEIN EH, GIAID A: Localization of urotensin-II immunoreactivity in normal human kidneys and renal carcinoma. J. Histochem. Cytochem. (2002) 50:885-889.
44. LANGHAM RG, GOW R, THOMSON NM, DOWLING JK, GILBERT RE: Increased expression of urotensin 2 and urotensin receptor GPR14 in human diabetic nephropathy. J. Am. Soc. Nephrol. (2003) 14:600A.
45. HELLER J, SCHEPKE M, NEEF M, WOITAS R, RABE C, SAUERBRUCH T: Increased urotensin II plasma levels in patients with cirrhosis and portal hypertension. J. Hepatol. (2002) 37:767-772.
46. TOTSUNE K, TAKAHASHI K, ARIHARA Z, SONE M, ITO S, MURAKAMI O: Increased plasma urotensin II levels in patients with diabetes mellitus. Clin. Sci. (2003) 104:1-5.
47. TOTSUNE K, TAKAHASHI K, ARIHARA Z et al.: Elevated plasma levels of immunoreactive urotensin II and its increased urinary excretion in patients with Type 2 diabetes mellitus: association with progress of diabetic nephropathy. Peptides (2004) 25:1809-1814.
48. WENYI Z, SUZUKI S, HIRAI M et al.: Role of urotensin II gene in genetic susceptibility to Type 2 diabetes mellitus in Japanese subjects. Diabetologia (2003) 46:972-976.
49. CAMARDA V, SONG W, MARZOLA E et al.: Urantide mimics urotensin-II induced calcium release in cells expressing recombinant UT receptors. Eur. J. Pharmacol. (2004) 498:83-86.
50. DHANAK D, NEEB MJ, DOUGLAS SA: Urotensin-II receptor modulators. Ann. Rep. Med. Chem. (2003) 38:99-110.
51. CROSTON GE, OLSSON R, CURRIER FA et al.: Discovery of the first nonpeptide agonist of the GPR14/urotensin-II receptor: 3-(4-chlorophenyl)-3-(2-(dimethylamino)ethyl)isochroman-1-one (AC-7954). J. Med. Chem. (2002) 45:4950-4953.
52. LEHMANN F, CURRIER, EA, OLSSON R, HACKSELL U, LUTHMAN K: Isochromanone-based urotensin-II receptor agonists. Bioorg. Med Chem. (2005) 13:3057-3068.
53. RAKOWSKI E, HASSAN G, DHANAK D, OHLSTEIN EH, DOUGLAS SA, GIAID A: A role for urotensin II in restenosis following balloon angioplasty: use of a selective UT receptor blocker. J. Mol. Cell. Cardiol. (2005) 39:785-791.
54. BOUSETTE N, OHLSTEIN EH, DHANAK D, DOUGLAS SA, GIAID A: Urotensin-II receptor blockade reduces mortality and improves congestive heart failure. Circulation (2005) 112:II-453.
55. DOUGLAS SA, BEHM DJ, AIYAR NV et al.: Nonpeptidic urotensin-II receptor antagonists I: in vitro pharmacological characterization of SB-706375. Br. J. Pharmacol. (2005) 145:620-635.
56. WATANABE T, SUGURO T, KANOME T et al.: Human urotensin II accelerates foam cell formation in human monocyte-derived macrophages. Hypertension (2005) 46:738-744.
57. CLOZEL M, BINKERT C, BIRKER-ROBACZEWSKA M et al.: Pharmacology of the urotensin-II receptor antagonist palosuran (ACT-058362; 1-[2-(4-benzyl- 4-hydroxy-piperidin-1-yl)- ethyl]- 3-(2-methyl-quinolin-4-yl)-urea sulfate salt): first demonstration of a pathophysiological role of the urotensin system. J. Pharmacol. Exp. Ther. (2004) 311:204-212.
58. CLOZEL M, HESS P, QIU C, DING S, REY M: The urotensin-II receptor antagonist palosuran improves pancreatic and renal function in diabetic rats. J. Pharmacol. Exp. Ther. (2005) 316:1115-1121.
59. JIN J, DHANAK D, KNIGHT SD et al.: Aminoalkoxybenzyl pyrrolidines as novel human urotensin-II receptor antagonists. Bioorg. Med. Chem. Lett. (2005) 15:3229-3232.
60. FLOHR S, KURZ M, KOSTENIS E, BRKOVICH A, FOURNIER A, KLABUNDE T. Identification of nonpeptidic urotensin II receptor antagonists by virtual screening based on a pharmacophore model derived from structure-activity relationship and nuclear magnetic resonance studies on urotensin II. J. Med. Chem. (2002) 45:1799-1805.
61. BEHM DJ, HARRISON SM, AO Z et al.: Deletion of the UT receptor gene results in the selective loss of urotensin-II contractile activity in aortae isolated from UT receptor knockout mice. Br. J. Pharmacol. (2003) 139:464-472.
62. BEHM DJ, HARRISON SM, DUDDY G et al.: Targeted gene deletion of the routine prepro-urotensin-II gene is associated with a lean phenotype and increased cardiac mass and vascular hyper-reactivity. Circulation (2005) 112:II-187.