卡培立肽是由三得利株式会社与宫崎医科大学共同研究合成、生产的由28个氨基酸构成的α型心房钠尿肽。

TargetValue NPR-A (Cell-free assay) 10.8 nM(EC50)

Carperitide (Atrial Natriuretic Peptide (ANP) (1-28), human, porcine) is a diuretic, natriuretic, and vasodilatory peptide hormone originally isolated from mammalian hearts. In cultured porcine endothelial cells the inhibition by porcine ANP (1-28) of immunoreactive endothelin-1 secretion after stimulation with Angiotensin II (Ang II) is paralleled by an increase in the cellular cGMP level. Porcine ANP (1-28) strongly inhibits immunoreactive endothelin-1 secretion in porcine aorta after stimulation with Ang II. ANP is a cardiac hormone involved in electrolyte and fluid homeostasis. The inhibition by ANP of endothelin-1 secretion stimulated by angiotensin II (ANGII) and thrombin using cultured human umbilical-vein endothelial cells. Human ANP (1-28) inhibits immunoreactive (ir)-endothelin-1 secretion and increases cyclic GMP in the human umbilical-vein endothelial cells. In glomeruli from normal rats, Human 125 I-ANP (1-28) binds to a single population of high affinity receptors with a mean equilibrium dissociation constant of 0.46 nM. Human ANP (1-28) binds to the glomerular ANP receptor with high affinity stimulated cGMP accumulation. Human ANP (1-28) markedly stimulates cGMP generation, but not cAMP generation in normal rat glomeruli.

Carperitide是一种有效的natriuretic peptide receptor (NPR)-A 激动剂，EC50值为10.8 nM。Carperitide用于治疗充血性心力衰竭。

药理学研究结果表明本药具有扩张血管、利尿作用，临床试验结果表明， 卡培立肽可减轻心脏前、后负荷，增加心脏输出量但不影响心率，对急性心力衰竭具有良好的治疗作用。卡培立肽是通过刺激心肌伸展，由心室内颗粒合成的，然后通过冠静脉分布全身，作用于血管平滑肌和肾脏等组织，调节血压和体内电解质平衡。