1998
DOI: 10.1097/00005344-199806000-00023
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Cardiovascular Effects of Nepicastat (RS-25560-197), a Novel Dopamine β-Hydroxylase Inhibitor

Abstract: Nepicastat (RS-25560-197) is a novel, selective, and potent inhibitor of dopamine beta-hydroxylase, which modulates catecholamine levels (reduces norepinephrine and elevates dopamine) in cardiovascular tissues. This study was designed to evaluate the cardiovascular effects of nepicastat. Acute oral administration of nepicastat (0.3, 1, 3, 10, and 30 mg/kg) produced attenuation of the pressor and positive chronotropic responses to preganglionic sympathetic nerve stimulation (about twofold to sixfold shift in th… Show more

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Cited by 8 publications
(2 citation statements)
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“…Hypertension is one of the most important risk factors for several cardiovascular diseases (CVDs) including heart failure, and coronary heart disease [1][2][3][4][5][6] . Several antihypertensive drugs including angiotensin-converting enzyme inhibitors (ACEi), angiotensin II receptor blockers (ARB), calcium channel blockers (CCB), beta-blockers, and diuretics are currently used for the treatment of hypertension [7][8][9] . A combination of antihypertensive drugs is in use to keep in mind the multiple targets these therapies achieve.…”
Section: Introductionmentioning
confidence: 99%
“…Hypertension is one of the most important risk factors for several cardiovascular diseases (CVDs) including heart failure, and coronary heart disease [1][2][3][4][5][6] . Several antihypertensive drugs including angiotensin-converting enzyme inhibitors (ACEi), angiotensin II receptor blockers (ARB), calcium channel blockers (CCB), beta-blockers, and diuretics are currently used for the treatment of hypertension [7][8][9] . A combination of antihypertensive drugs is in use to keep in mind the multiple targets these therapies achieve.…”
Section: Introductionmentioning
confidence: 99%
“…Interest in the development of inhibitors of dopamine β-hydroxylase (DβH; EC 1.14.17.1; dopamine β-monooxygenase) has centered on the hypothesis that inhibition of this enzyme may provide significant clinical improvements in patients suffering from cardiovascular disorders such as hypertension or congestive heart failure (Beliaev et al, 2006;Bonifácio et al, 2009;Hegde and Friday, 1998;Ishii et al, 1975;Kruse et al, 1987;Ohlstein et al, 1987;Sabbah et al, 2000;Stanley et al, 1998). The rationale for the use of DβH inhibitors is based on their capacity to inhibit the biosynthesis of noradrenaline, which is achieved via enzymatic hydroxylation of dopamine (Gomes and Soares-da-Silva, 2008;Jose et al, 2002;Jose et al, 2010;Soares-da-Silva, 1986, 1987.…”
Section: Introductionmentioning
confidence: 99%