Blood pressure-decreasing effect of etamicastat alone and in combination with antihypertensive drugs in the spontaneously hypertensive rat

Hypertension Research

Volumn 38, Issue 1, 2015, Pages 30-38

  Igreja, Bruno ^a   Pires, Nuno Miguel ^a   Bonifácio, Maria João ^a   Loureiro, Ana Isabel ^a   Fernandes Lopes, Carlos ^a   Wright, Lyndon Christopher ^a   Soares Da Silva, Patrício ^a,b,c  

^a DEPARTMENT OF RESEARCH AND DEVELOPMENT   (Portugal)

^b University of Porto   (Portugal)

^c UNIVERSITY OF PORTO   (Portugal)

Author keywords

blood pressure; noradrenaline; sympathetic nervous system

Indexed keywords

ANTIHYPERTENSIVE AGENT; CAPTOPRIL; CATECHOLAMINE; DILTIAZEM; DOPAMINE; ETAMICASTAT; HYDROCHLOROTHIAZIDE; LOSARTAN; METOPROLOL; NORADRENALIN; PRAZOSIN; BENZOPYRAN DERIVATIVE; IMIDAZOLE DERIVATIVE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIHYPERTENSIVE THERAPY; AREA UNDER THE CURVE; ARTICLE; BLOOD PRESSURE; CATECHOLAMINE BLOOD LEVEL; CONTROLLED STUDY; DRUG EFFICACY; ESSENTIAL HYPERTENSION; FRONTAL CORTEX; HALF LIFE TIME; HEART FUNCTION; HYPERTENSION; KIDNEY FUNCTION; MALE; MAXIMUM PLASMA CONCENTRATION; MONOTHERAPY; NONHUMAN; RAT; SPONTANEOUSLY HYPERTENSIVE RAT; TACHYCARDIA; ANIMAL; BLOOD; DISEASE MODEL; DOSE RESPONSE; DRUG COMBINATION; DRUG EFFECTS; DRUG SCREENING; KIDNEY; METABOLISM;

ANIMALS; ANTIHYPERTENSIVE AGENTS; BENZOPYRANS; BLOOD PRESSURE; CATECHOLAMINES; DISEASE MODELS, ANIMAL; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG EVALUATION, PRECLINICAL; DRUG THERAPY, COMBINATION; HYPERTENSION; IMIDAZOLES; KIDNEY; MALE; RATS, INBRED SHR;

EID: 84920541004     PISSN: 09169636     EISSN: 13484214     Source Type: Journal    
DOI: 10.1038/hr.2014.143     Document Type: Article

References (55)

1. Kearney PM, Whelton M, Reynolds K, Muntner P, Whelton PK, He J. Global burden of hypertension: analysis of worldwide data. Lancet 2005; 365: 217-223
2. Calhoun DA, Jones D, Textor S, Goff DC, Murphy TP, Toto RD, White A, Cushman WC, White W, Sica D, Ferdinand K, Giles TD, Falkner B, Carey RM. Resistant hypertension: diagnosis, evaluation, and treatment. A scientific statement from the American Heart Association Professional Education Committee of the Council for High Blood Pressure Research. Hypertension 2008; 51: 1403-1419
3. Malpas SC. Sympathetic nervous system overactivity and its role in the development of cardiovascular disease. Physiol Rev 2010; 90: 513-557
4. Mancia G, Fagard R, Narkiewicz K, Redón J, Zanchetti A, Böhm M, Christiaens T, Cifkova R, De Backer G, Dominiczak A, Galderisi M, Grobbee DE, Jaarsma T, Kirchhof P, Kjeldsen SE, Laurent S, Manolis AJ, Nilsson PM, Ruilope LM, Schmieder RE, Sirnes PA, Sleight P, Viigimaa M, Waeber B, Zannad F, Task Force Members. 2013 ESH/ESC Guidelines for the management of arterial hypertension: the Task Force for the management of arterial hypertension of the European Society of Hypertension (ESH) and of the European Society of Cardiology (ESC). J Hypertens 2013; 31: 1281-1357
5. Grassi G. Sympathetic neural activity in hypertension and related diseases. Am J Hypertens 2010; 23: 1052-1060
6. Grassi G, Seravalle G, Quarti-Trevano F. The 'neuroadrenergic hypothesis' in hypertension: current evidence. Exp Physiol 2010; 95: 581-586
7. Esler M, Kaye D. Sympathetic nervous system activation in essential hypertension, cardiac failure and psychosomatic heart disease. J Cardiovasc Pharmacol 2000; 35 (Suppl 4): S1-S7
8. Parati G, Esler M. The human sympathetic nervous system: its relevance in hypertension and heart failure. Eur Heart J 2012; 33: 1058-1066
9. Grassi G, Bolla G, Quarti-Trevano F, Arenare F, Brambilla G, Mancia G. Sympathetic activation in congestive heart failure: reproducibility of neuroadrenergic markers. Eur J Heart Fail 2008; 10: 1186-1191
10. Lee CS, Tkacs NC. Current concepts of neurohormonal activation in heart failure: mediators and mechanisms. AACN Adv Crit Care 2008; 19: 364-385
11. Mancia G, Grassi G, Giannattasio C, Seravalle G. Sympathetic activation in the pathogenesis of hypertension and progression of organ damage. Hypertension 1999; 34(Pt 2): 724-728
12. Krum H, Schlaich M, Whitbourn R, Sobotka PA, Sadowski J, Bartus K, Kapelak B, Walton A, Sievert H, Thambar S, Abraham WT, Esler M. Catheter-based renal sympathetic denervation for resistant hypertension: a multicentre safety and proof-ofprinciple cohort study. Lancet 2009; 373: 1275-1281
13. Esler MD, Krum H, Sobotka PA, Schlaich MP, Schmieder RE, Bohm M. Renal sympathetic denervation in patients with treatment-resistant hypertension (The Symplicity HTN-2 Trial): a randomised controlled trial. Lancet 2010; 376: 1903-1909
14. Worthley SG, Tsioufis CP, Worthley MI, Sinhal A, Chew DP, Meredith IT, Malaiapan Y, Papademetriou V. Safety and efficacy of a multi-electrode renal sympathetic denervation system in resistant hypertension: the EnligHTN I trial. Eur Heart J 2013; 34: 2132-2140
15. Mahfoud F, Ukena C, Schmieder RE, Cremers B, Rump LC, Vonend O, Weil J, Schmidt M, Hoppe UC, Zeller T, Bauer A, Ott C, Blessing E, Sobotka PA, Krum H, Schlaich M, Esler M, Böhm M. Ambulatory blood pressure changes after renal sympathetic denervation in patients with resistant hypertension. Circulation 2013; 128: 132-140
16. Krum H, Schlaich MP, Sobotka PA, Bohm M, Mahfoud F, Rocha-Singh K, Katholi R, Esler MD. Percutaneous renal denervation in patients with treatment-resistant hypertension: final 3-year report of the Symplicity HTN-1 study. Lancet 2013; 383: 622-629
17. Mahfoud F, Luscher TF, Andersson B, Baumgartner I, Cifkova R, Dimario C, Doevendans P, Fagard R, Fajadet J, Komajda M, Lefèvre T, Lotan C, Sievert H, Volpe M, Widimsky P, Wijns W, Williams B, Windecker S, Witkowski A, Zeller T, Böhm M, European Society of Cardiology. Expert consensus document from the European Society of Cardiology on catheter-based renal denervation. Eur Heart J 2013; 34: 2149-2157
18. Hayek SS, Abdou MH, Demoss BD, Legaspi JM, Veledar E, Deka A, Krishnan SK, Wilmot KA, Patel AD, Kumar VR, Devireddy CM. Prevalence of resistant hypertension and eligibility for catheter-based renal denervation in hypertensive outpatients. Am J Hypertens 2013, 1452-1458
19. Stanley WC, Li B, Bonhaus DW, Johnson LG, Lee K, Porter S, Walker K, Martinez G, Eglen RM, Whiting RL, Hegde SS. Catecholamine modulatory effects of nepicastat (RS-25560-197), a novel, potent and selective inhibitor of dopamine-beta-hydroxylase. Br J Pharmacol 1997; 121: 1803-1809
20. Bertera FM, Del Mauro JS, Lovera V, Chiappetta D, Polizio AH, Taira CA, Höcht C. Acute effects of third generation beta-blockers on short-Term and beat-To-beat blood pressure variability in sinoaortic-denervated rats. Hypertens Res 2013; 36: 349-355
21. Hegde SS, Friday KF. Dopamine-beta-hydroxylase inhibition: a novel sympathomodulatory approach for the treatment of congestive heart failure. Curr Pharm Des 1998; 4: 469-479
22. Soares-da-Silva P. Evidence for a non-precursor dopamine pool in noradrenergic neurones of the dog mesenteric artery. Naunyn Schmiedebergs Arch Pharmacol 1986; 333: 219-223
23. Soares-da-Silva P. A comparison between the pattern of dopamine and noradrenaline release from sympathetic neurones of the dog mesenteric artery. Br J Pharmacol 1987; 90: 91-98
24. Gomes P, Soares-da-Silva P. Dopamine. In Michael Bader (ed.). Cardiovascular Hormone Systems: From Molecular Mechanisms to Novel Therapeutics. Wiley-Blackwell: Weinheim, Germany. 2008, pp 251-293
25. Jose PA, Eisner GM, Felder RA. Role of dopamine receptors in the kidney in the regulation of blood pressure. Curr Opin Nephrol Hypertens 2002; 11: 87-92
26. Jose PA, Soares-da-Silva P, Eisner GM, Felder RA. Dopamine and G protein-coupled receptor kinase 4 in the kidney: role in blood pressure regulation. Biochim Biophys Acta 2010; 1802: 1259-1267
27. Ishii Y, Fujii Y, Mimura C, Umezawa H. Pharmacological action of FD-008, a new dopamine beta-hydroxylase inhibitor. I. Effects on blood pressure in rats and dogs. Arzneimittelforschung 1975; 25: 55-59
28. Kruse LI, Kaiser C, DeWolf WE Jr, Frazee JS, Ross ST, Wawro J, Wise M, Flaim KE, Sawyer JL, Erickson RW. Multisubstrate inhibitors of dopamine beta-hydroxylase. 2. Structure-Activity relationships at the phenethylamine binding site. J Med Chem 1987; 30: 486-494
29. Ohlstein EH, Kruse LI, Ezekiel M, Sherman SS, Erickson R, DeWolf WE Jr, Berkowitz BA. Cardiovascular effects of a new potent dopamine beta-hydroxylase inhibitor in spontaneously hypertensive rats. J Pharmacol Exp Ther 1987; 241 (2): 554-559
30. Kruse LI, Kaiser C, DeWolf WE Jr, Frazee JS, Erickson RW, Ezekiel M, Ohlstein EH, Ruffolo RR Jr, Berkowitz BA. Substituted 1-benzylimidazole-2-Thiols as potent and orally active inhibitors of dopamine beta-hydroxylase. J Med Chem 1986; 29: 887-889
31. Falcao A, Nunes T, Rocha JF, Almeida L, Soares-da-Silva P. Comparative bioavailability study of etamicastat (BIA 5-453) under fasted and fed conditions. J Clin Pharmacol 2009; 49: 1095 (abstract
32. Nunes T, Rocha JF, Vaz-da-Silva M, Falcao A, Almeida L, Soares-da-Silva P. Pharmacokinetics and tolerability of etamicastat following single and repeated administration in elderly versus young healthy male subjects: an open-label, single-center, parallel-group study. Clin Ther 2011; 33: 776-791
33. Nunes T, Rocha JF, Vaz-da-Silva M, Igreja B, Wright LC, Falcão A, Almeida L, Soares-da-Silva P. Safety, tolerability, and pharmacokinetics of etamicastat, a novel dopamine-beta-hydroxylase inhibitor, in a rising multiple-dose study in young healthy subjects. Drugs R D 2010; 10: 225-242
34. Rocha JF, Vaz-da-Silva M, Nunes T, Igreja B, Loureiro AI, Bonifácio MJ, Wright LC, Falcão A, Almeida L, Soares-da-Silva P. Single-dose tolerability, pharmacokinetics, and pharmacodynamics of etamicastat (BIA 5-453), a new dopamine {beta}-hydroxylase inhibitor, in healthy subjects. J Clin Pharmacol 2012; 52: 156-170
35. Vaz-da-Silva M, Nunes T, Rocha JF, Falcao A, Almeida L, Soares-da-Silva P. Effect of food on the pharmacokinetic profile of etamicastat (BIA 5-453). Drugs R D 2011; 11: 127-136
36. Beliaev A, Learmonth DA, Soares-da-Silva P. Synthesis and biological evaluation of novel, peripherally selective chromanyl imidazolethione-based inhibitors of dopamine beta-hydroxylase. J Med Chem 2006; 49: 1191-1197
37. Bonifácio MJ, Igreja B, Wright L, Soares-da-Silva P. Kinetic studies on the inhibition of dopamine-β-hydroxylase by BIA 5-453. pA2 Online 2009; 7: 050P (abstract
38. Almeida L, Nunes T, Costa R, Rocha JF, Vaz-da-Silva M, Soares-da-Silva P. Etamicastat, a novel dopamine beta-hydroxylase inhibitor: tolerability, pharmacokinetics, and pharmacodynamics in patients with hypertension. Clin Ther 2013; 35: 1983-1996
39. Loureiro AI, Fernandes-Lopes C, Bonifacio MJ, Wright LC, Soares-da-Silva P. N-Acetylation of etamicastat, a reversible dopamine-beta-hydroxylase inhibitor. Drug Metab Dispos 2013; 41: 2081-2086
40. Soares-da-Silva P, Pestana M, Vieira-Coelho MA, Fernandes MH, Albino-Teixeira A. Assessment of renal dopaminergic system activity in the nitric oxide-deprived hypertensive rat model. Br J Pharmacol 1995; 114: 1403-1413
41. Huetteman DA, Bogie H. Direct blood pressure monitoring in laboratory rodents via implantable radio telemetry. Methods Mol Biol 2009; 573: 57-73
42. Clough DP, Hatton R, Keddie JR, Collis MG. Hypotensive action of captopril in spontaneously hypertensive and normotensive rats. Interference with neurogenic vasoconstriction. Hypertension 1982; 4: 764-772
43. Narita H, Nagao T, Yabana H, Yamaguchi I. Hypotensive and diuretic actions of diltiazem in spontaneously hypertensive and Wistar Kyoto rats. J Pharmacol Exp Ther 1983; 227: 472-477
44. Wada T, Sanada T, Ojima M, Kanagawa R, Nishikawa K, Inada Y. Combined effects of the angiotensin II antagonist candesartan cilexetil (TCV-116) and other classes of antihypertensive drugs in spontaneously hypertensive rats. Hypertens Res 1996; 19: 247-254
45. DePasquale MJ, Fossa AA, Holt WF, Mangiapane ML. Central DuP 753 does not lower blood pressure in spontaneously hypertensive rats. Hypertension 1992; 19(Part 2): 668-671
46. Antonaccio MJ, High J, DeForrest JM, Sybertz E. Antihypertensive effects of 12 beta adrenoceptor antagonists in conscious spontaneously hypertensive rats: relationship to changes in plasma renin activity, heart rate and sympathetic nerve function. J Pharmacol Exp Ther 1986; 238: 378-387
47. Ryan MJ, Bjork FA, Cohen DM, Coughenour LL, Major TC, Mathias NP, Mertz TE, Olszewski BJ, Singer RM, Evans DB CI-926 (3-[4-[4-(3-methylphenyl)-1-piperazinyl] butyl]-2, 4-imidazolinedione): antihypertensive profile and pharmacology. J Pharmacol Exp Ther 1986; 238: 473-479
48. Jose PA, Eisner GM, Felder RA. Dopamine and the kidney: a role in hypertension?. Curr Opin Nephrol Hypertens 2003; 12: 189-194
49. Igreja B, Wright L, Soares-da-Silva P. Sustained antihypertensive effects of a selective peripheral dopamine-β-hydroxylase inhibitor. Hypertension 2007; 50: E133 (abstract
50. Foss JD, Fink GD, Osborn JW. Reversal of genetic salt-sensitive hypertension by targeted sympathetic ablation. Hypertension 2013; 61: 806-811
51. Pfeffer MA, Stevenson LW. Beta-Adrenergic blockers and survival in heart failure. New Engl J Med 1996; 334: 1396-1397
52. Goldsmith SR. Interactions between the sympathetic nervous system and the RAAS in heart failure. Curr Heart Fail Rep 2004; 1: 45-50
53. Kalra S, Kalra B, Agrawal N. Combination therapy in hypertension: an update. Diabetol Metab Syndr 2010; 2: 44
54. Law MR, Morris JK, Wald NJ. Use of blood pressure lowering drugs in the prevention of cardiovascular disease: meta-Analysis of 147 randomised trials in the context of expectations from prospective epidemiological studies. BMJ 2009; 338: b1665
55. Fagard RH, Celis H, Thijs L, Staessen JA, Clement DL, De Buyzere ML, De Bacquer DA. Daytime and nighttime blood pressure as predictors of death and cause-specific cardiovascular events in hypertension. Hypertension 2008; 51: 55-61