Nesiritide

Nesiritide (Brain Natriuretic Peptide-32 human) is a recombinant human B-type natriuretic peptide. Nesiritide is a NPRs agonist, with K_d values of 7.3 and 13 pM for NPR-A and NPR-C, respectively. Nesiritide regulates V_1/2 activation/inactivation of the L-type calcium channel. Nesiritide shows vasodilatory, diuretic, and natriuretic activities. Nesiritide is used in cardiovascular diseases such as heart failure and vascular remodeling after arterial injury^{[1][2][3][4][5][6][7]}. IC50 & Target:Kd: 7.3 Pm (NPR-A), 13 pM (NPR-C)^[1]. In Vitro:Nesiritide (1 nM-1 μM) significantly decreases cell shortening in ventricular myocytes isolated from rat hearts in a dose-dependent manner^[1].
Nesiritide (1 μM) increases the V_1/2 activation of the L-type calcium channel by 51.1% and decreases V_1/2 inactivation by 31.8% in ventricular myocytes isolated from rat hearts^[1].
In Vivo:Nesiritide (2 μg/kg i.v. bolus followed by 0.01 μg/kg/min i.v. infusion) reduces infarct size, preserves endothelial function, and lessens lung edema in a porcine model of acute coronary occlusion simulating urgent CABG surgery^[2].
Nesiritide (0.1 mg/kg/day; s.c.; once daily; 4 weeks) protects endothelial function after balloon-induced trauma in the iliac artery in rabbits^[3].