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Chemical Structure| 106730-54-5 Chemical Structure| 106730-54-5

Structure of Olprinone
CAS No.: 106730-54-5

Chemical Structure| 106730-54-5

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Olprinone is a selective phosphodiesterase 3 (PDE3) inhibitor.

Synonyms: Loprinone

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Product Details of Olprinone

CAS No. :106730-54-5
Formula : C14H10N4O
M.W : 250.26
SMILES Code : N#CC1=CC(C2=CN3C(C=C2)=NC=C3)=C(C)NC1=O
Synonyms :
Loprinone
MDL No. :MFCD25541649
InChI Key :JPAWFIIYTJQOKW-UHFFFAOYSA-N
Pubchem ID :4593

Safety of Olprinone

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Rabbit coronary artery smooth muscle cells 100 µM 15 minutes To investigate the effects of olprinone on acetylcholine (ACh)-induced membrane potential and contraction. Results showed that olprinone hyperpolarized the resting membrane and attenuated the ACh-induced contraction. Br J Pharmacol. 2000 Mar;129(5):1000-6
Human coronary artery endothelial cells 0.004 mM 60 minutes Evaluate cytotoxicity of Olprinone on human coronary artery endothelial cells, results showed no cytotoxicity Int J Mol Sci. 2023 Jun 29;24(13):10850
Rat smooth muscle cells 0.004 mM 60 minutes Evaluate cytotoxicity of Olprinone on rat smooth muscle cells, results showed no cytotoxicity Int J Mol Sci. 2023 Jun 29;24(13):10850
Primary cultured rat hepatocytes 0.2-1 mM 8 hours OLP dose-dependently inhibited IL-1β-stimulated iNOS induction and NF-κB activation, reducing NO production. Int J Mol Sci. 2024 Jun 29;25(13):7189

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rat Rat abdominal aorta Local administration 0.004 mM Measured after 10 minutes Evaluate vasodilatory effects of Olprinone on rat abdominal aorta, results showed maximal vasodilation effect Int J Mol Sci. 2023 Jun 29;24(13):10850
Mice Spinal cord injury model Intraperitoneal injection 0.2 mg/kg Administered at 1 and 6 hours post-injury, continued daily until day 9 Olprinone significantly attenuated the inflammatory response and tissue injury after spinal cord trauma, reducing neutrophil infiltration, nitrotyrosine formation, pro-inflammatory cytokines, NF-κB expression, p-ERK1/2 and p38 expression, and apoptosis (TUNEL staining, FAS ligand, Bax and Bcl-2 expression). Additionally, Olprinone significantly improved the recovery of hind-limb function. PLoS One. 2010 Sep 7;5(9):e12170
C57BL/6J mice Alcohol intake and preference model Oral 0.5 mg/kg Once daily for up to 10 days To evaluate the effect of Olprinone on alcohol intake and preference; results showed no significant effect of Olprinone on ethanol consumption or preference Front Neurosci. 2014 May 27;8:129
New Zealand white rabbits Acute respiratory distress syndrome (ARDS) model Intravenous 1 mg/kg Single dose, lasting 4 hours Olprinone treatment reduced the release of inflammatory mediators and markers of oxidative damage, decreased apoptosis of epithelial cells, and improved respiratory parameters. Int J Mol Sci. 2020 May 11;21(9):3382
Sprague-Dawley (SD) rats 70% partial hepatectomy and lipopolysaccharide treatment (PH/LPS) model Intraperitoneal injection 10 mg/kg Single dose, observed for 120 hours OLP significantly increased the survival rate (85.7%) of PH/LPS-treated rats, reduced TNF-α, CXCL1, and iNOS mRNA expression in the liver, and suppressed nuclear translocation and/or DNA binding ability of NF-κB. Int J Mol Sci. 2024 Jun 29;25(13):7189

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