Milrinone

SKU: orb1224003

Description

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.\n(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.

Key Properties

• CAS Number: 78415-72-2
• MW: 211.22
• Purity: >98% (HPLC)
• Formula: C₁₂H₉N₃O
• SMILES: N#CC1=CC(C2=CC=NC=C2)=C(C)NC1=O
• Target: PDE
• Solubility: DMSO: 42 mg/mL (198.84 mM)

Bioactivity

• 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.
• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

WIN 47,203

Quick Database Links

Gene Symbol

PDE