Nesiritide CAS:124584-08-3

Nesiritid, sold under the brand name Natrecor, er den rekombinante formen av 32 aminosyre humant B-type natriuretisk peptid, som normalt produseres av det ventrikulære myokardiet. Nesiritide works to facilitate cardiovascular fluid homeostasis through counterregulation of the renin–angiotensin–aldosterone system, stimulerer syklisk guanosinmonofosfat, fører til avslapning av glatte muskelceller.

Nesiritide was believed initially to be beneficial for acute decompensated congestive heart failure. Den fikk godkjenning fra USAs Food and Drug Administration for dette formålet i 2001 etter første manglende godkjenning. I juli 2011, the results of the largest study so far for nesiritide was published in The New England Journal of Medicine. The study failed to show a difference between nesiritide and placebo on mortality or re-hospitalizations.

Nesiritide is a medication used to treat acutely decompensated congestive heart failure with dyspnea at rest or with minimal exertion (such as talk, eating or bathing). Nesiritide is a 32 amino acid recombinant human B-type natriuretic peptide.

Human BNP binds to the particulate guanylate cyclase receptor of vascular smooth muscle and endothelial cells, leading to increased intracellular concentrations of guanosine 3'5'-cyclic monophosphate (cGMP) and smooth muscle cell relaxation. Cyclic GMP serves as a second messenger to dilate veins and arteries. Nesiritide has been shown to relax isolated human arterial and venous tissue preparations that were precontracted with either endothelin-1 or the alpha-adrenergic agonist, phenylephrine. In human studies, nesiritide produced dose-dependent reductions in pulmonary capillary wedge pressure (PCWP) and systemic arterial pressure in patients with heart failure. In animals, nesiritide had no effects on cardiac contractility or on measures of cardiac electrophysiology such as atrial and ventricular effective refractory times or atrioventricular node conduction. Naturally occurring atrial natriuretic peptide (ANP), a related peptide, increases vascular permeability in animals and humans and may reduce intravascular volume. The effect of nesiritide on vascular permeability has not been studied.