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Inhibition of NEP with phosphoramidon increased flare intensity (P < 0.002) and size (P < 0.01), while blocking ACE had no effect on neurogenic vasodilation. CGRP release could be measured in microdialysis samples after phosphoramidon perfusion only (P < 0.03), not in samples with captopril or saline perfusion.
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Valsartan/sacubitril is the first of a new class of drugs that have been referred to as angiotensin receptor-neprilysin inhibitors. 3 The class name is a misnomer because ARBs are not enzyme inhibitors. A more accurate name for the class would be angiotensin receptor antagonist/neprilysin inhibitors.
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CNP has the shortest half-life (2.6 min.) of all the natriuretic peptides in humans [ 29] and a similarly low half-life (1.6 min.) in sheep [ 30 ]. When CNP was infused in sheep at rates of 1 or 10 pmol/kg/min, metabolic clearance rates of 3.1 and 2.5 l/min, respectively, were observed. Like ANP, CNP is removed in dogs by the lungs, kidney and.
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Natriuretic peptides (NPs) are peptide hormones that are synthesized by the heart, brain, and other organs. The release of these peptides by the heart is stimulated by atrial and ventricular distension, as well as by neurohumoral stimuli, usually in response to heart failure. The main physiological actions of natriuretic peptides are to reduce.
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Neprilysin (NEP) is a ubiquitous membrane-bound zinc-dependent metalloprotease that hydrolyzes numerous regulatory peptides including vasoactive peptides such as natriuretic peptides, adrenomedullin, angiotensins I and II, bradykinin, and endothelin-1 as well as non-vasoactive peptides such as beta amyloid, glucagon, enkephalins, and substance P.
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Vasopeptidase inhibitors represent a new class of cardiovascular drugs. They function as a combined angiotensin-converting enzyme (ACE) inhibitor and neutral endopeptidase (NEP) inhibitor, the latter of which potentiates the actions of atrial natriuretic peptide (ANP) by minimizing its degradation in the circulation.
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Bestatin, a small molecular weight dipeptide, is a potent inhibitor of various aminopeptidases as well as LTA4 hydrolase. Various physiological functions of Bestatin have been identified, viz.: (1) an immunomodifier for enhancing the proliferation of normal human bone marrow granulocyte-macrophage progenitor cells to form CFU-GM colonies; Bestatin exerts a direct stimulating effect on.
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The peak of CD10/NEP transcript levels in human foetus was identified at 11-13 weeks of gestation and localized to epithelial cells and mesenchyme of developing airways suggesting that NEP plays an important role in lung development (Sunday et al., 1992).It was later confirmed that NEP regulates foetal lung growth and maturation by mediating endogenous bombesin-like peptides (King et al., 1997).
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Introduction. The renin-angiotensin-aldosterone system plays an important role in regulating blood pressure (BP) and is a key factor underlying the development of hypertension, with major clinical guidelines recommending inhibition of this system as one of the first-line drugs, along with other drugs including calcium channel blockers and diuretics. 1 Clinically, this is achieved with ACE.
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N-Ethylpentylone (NEP) is one of the most confiscated synthetic cathinones in the world. However, its pharmacology and pharmacokinetics remain largely unknown. In this study, the pharmacokentics of NEP in rat nucleus accumbens (NAc) was assessed via brain microdialysis after the intraperitoneal (ip).
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Moreover, it should be underlined that the expression level of NEP is dependent on the proliferation and differentiation status of tumor cells. NEP is implicated both indirectly and directly in the regulation of signaling pathways. Its indirect action involves proteolytic degradation or activation of bioactive peptides, growth factors, and.
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NEP = neprilysin. Neprilysin has putative roles in the modulation of peptides implicated in the cardiovascular system and in other systems related to amyloid deposition, opioid receptor and pain processing, gastrointestinal processes, metabolism, sperm motility, and skin aging.
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In lymphocytes, NEP expression is developmentally regulated. 61,64. NEP hydrolyses Ang I to angiotensin 1-7, and since Ang 1-7 counters the action of the vasoconstrictor Ang II, the hydrolysis of Ang I to Ang 1-7 by NEP produces a potentially beneficial BP-lowering effect. Also desirable, NEP catabolizes the potent vasoconstrictor ET-1.
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Neuropathic pain (NeP) can result from sources as varied as nerve compression, channelopathies, autoimmune disease, and incision. By identifying the neurobiological changes that underlie the pain state, it will be clinically possible to exploit mechanism-based therapeutics for maximum analgesic effect as diagnostic accuracy is optimized. Obtaining sufficient knowledge regarding the.
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Neprilysin (NEP) is a zinc-dependent metalloproteinase that exists in organisms in both transmembrane and soluble forms. NEP substrates are involved in regulating the cardiovascular and nervous systems. In this review, we discuss some of the biochemical characteristics and physiological functions of.