Aliskiren: An orally active renin inhibitor
نویسندگان
چکیده
منابع مشابه
Aliskiren: A Novel, Orally Active Renin Inhibitor
Renin-angiotensin-aldosterone systems play a major role in the regulation of human homeostasis mechanism, which are also involved in the development of hypertension and end-organ damage through activation of angiotensin II. Inhibitors of the renin-angiotensin-aldosterone system may reduce the development of end-organ damage to a greater extent than other antihypertensive agents. Aliskiren is th...
متن کاملAn orally active inhibitor of renin.
A potent renin inhibitor, U-71038 (Boc-Pro-Phe-N-MeHis-Leu psi[CHOHCH2]Val-Ile-Amp), was tested for oral effectiveness. Enzyme kinetic studies indicated that U-71038 was a competitive inhibitor of hog renin with an inhibitor constant (Ki) value of 12 nM. Intravenous as well as oral administration of U-71038 to anesthetized, ganglion-blocked rats infused with hog renin elicited dose-related hypo...
متن کاملAngiotensin II suppression in humans by the orally active renin inhibitor Aliskiren (SPP100): comparison with enalapril.
Renin is the main determinant of angiotensin (Ang) II levels. It, therefore, always appeared desirable to reduce Ang II levels by direct inhibition of renin. So far, specific renin inhibitors lacked potency and/or oral availability. We tested the new orally active nonpeptidic renin inhibitor SPP100 (Aliskiren, an octanamide with a 50% inhibitory concentration [IC50] in the low nanomolar range) ...
متن کاملES-8891, an orally active inhibitor of human renin.
A newly synthesized orally active renin inhibitor, N-morpholinoacetyl-(1-naphthyl)-L-alanyl-(4-thiazolyl)-L-alanyl (3S,4S)-4-amino-3-hydroxy-5-cyclohexylpentanoyl-n-hexylamide (ES-8891), was found to be a highly potent competitive inhibitor of human renin with an inhibition constant of 1.1 nM. This inhibitor was also active against monkey renin, although there was less inhibition of renin in pi...
متن کاملAliskiren – an orally active renin inhibitor. Review of pharmacology, pharmacodynamics, kinetics, and clinical potential in the treatment of hypertension
The importance of renin-angiotensin-aldosterone system (RAAS) in diseases such as hypertension, congestive heart failure and chronic renal failure has long ago been recognized. It has also been established that inhibition of RAAS, using inhibitors of the angiotensin-converting enzyme (ACE) or angiotensin II receptor blockers (ARB), is an effective way to intervene with the pathogenesis of these...
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ژورنال
عنوان ژورنال: Journal of Pharmacy and Bioallied Sciences
سال: 2011
ISSN: 0975-7406
DOI: 10.4103/0975-7406.80764