Milrinone

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Milrinone (Win 47203) 是一种 PDE3 抑制剂，可增加细胞内环磷酸腺苷，从而改善心室功能和血管舒张。

Milrinone(Win 47203) is a PDE3 inhibitor that increases intracellular cyclic adenosine monophosphate resulting in improved ventricular function and vasodilation.(In Vitro):Milrinone (1 μM) increases PKA activity in hypoxic myocytes to normoxic levels. Milrinone (50 nM) normalizes TP receptor sensitivity in hypoxic myocytes by restoring PKA-mediated regulatory TP receptor phosphorylation. Milrinone significantly reduces NE-induced vasoconstriction, attenuating both NE sensitivity and maximal tension generation. Inhibition of ATP-sensitive K+ channels or voltage-gated K+ channels do not prevent the milrinone-induced attenuation of NE responses. (In Vivo):Milrinone (1 μg/kg/min, i.v.) significantly reduces PAP, PVR (?18.96 ± 1.7%), and LAP (?26.03 ± 2.3%) in congestive heart failure (CHF) rats. Milrinone (1 mg/mL, inhalation) results in a near-maximal reduction of PAP without significant effects on AP, decreases pulmonary artery pressure similarly in a larger collective of CHF rats. Milrinone inhalation selectively increases cAMP but not cGMP plasma concentrations in both groups. Repeated milrinone inhalations even reduce lung wet/dry weight ratio. Milrinone (49.5 μg) largely shifts the ESPVR upwards and significantly increases end-systolic pressure (ESP(0.08)) and the systolic pressure-volume area (PVA(0.08)) at a mid-range LV volume (0.08 mL/g myocardium). Milrinone also slightly decreases LV ESP(ESV) and decreased Ea.

Milrinone (1 μM) increases PKA activity in hypoxic myocytes to normoxic levels. Milrinone (50 nM) normalizes TP receptor sensitivity in hypoxic myocytes by restoring PKA-mediated regulatory TP receptor phosphorylation. Milrinone significantly reduces NE-induced vasoconstriction, attenuating both NE sensitivity and maximal tension generation. Inhibition of ATP-sensitive K+ channels or voltage-gated K+ channels do not prevent the milrinone-induced attenuation of NE responses.

Milrinone (1 μg/kg/min, i.v.) significantly reduces PAP, PVR (?18.96 ± 1.7%), and LAP (?26.03 ± 2.3%) in congestive heart failure (CHF) rats. Milrinone (1 mg/mL, inhalation) results in a near-maximal reduction of PAP without significant effects on AP, decreases pulmonary artery pressure similarly in a larger collective of CHF rats. Milrinone inhalation selectively increases cAMP but not cGMP plasma concentrations in both groups. Repeated milrinone inhalations even reduce lung wet/dry weight ratio. Milrinone (49.5 μg) largely shifts the ESPVR upwards and significantly increases end-systolic pressure (ESP(0.08)) and the systolic pressure-volume area (PVA(0.08)) at a mid-range LV volume (0.08 mL/g myocardium). Milrinone also slightly decreases LV ESP(ESV) and decreased Ea.

WIN 47,203

Angiogenesis

PDE

PDE2| PDE3

Cardiovascular Disease

——

78415-72-2

211.22

C12H9N3O

>98% (HPLC)

DMSO: 42 mg/mL (198.84 mM)

N#CC1=CC(C2=CC=NC=C2)=C(C)NC1=O

6-methyl-2-oxo-5-pyridin-4-yl-1H-pyridine-3-carbonitrile

(-20℃)

With Ice Pack

≥ 2 years