Pelrinone
Pelrinone is an orally active cardiotonic agent and PDE III inhibitor with an IC50 of 36 μM. Pelrinone elevates intracellular cAMP levels. The action of Pelrinone is independent of β-adrenergic receptors, and it does not inhibit Na+/K+-ATPase. Pelrinone exerts positive inotropic and vasodilatory effects. Pelrinone inhibits platelet aggregation, reduces thrombus formation, and exerts weak anticoagulant activity without altering hematocrit or circulating platelet counts. Pelrinone can be used in research related to congestive heart failure and coronary thrombosis.
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- No. CAS: 94386-65-9
- Fòrmula: C12H11N5O
- Peso molecular:241.25
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Actividad biológica
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PDE Ⅲ 36 μM (IC50) |
Pelrinone inhibits PDE in crude bovine heart extracts with an IC50 of 76 μM; it also inhibits purified bovine heart PDE component III with an IC50 of 36 μM, exhibiting stronger activity against the cAMP-specific component III isozyme[1].
Pelrinone (at different concentrations; pre-incubated for 3 min) inhibits platelet-rich plasma aggregation induced by Arachidonic acid (HY-109590), U46619 (HY-108566), Collagen, phase II adrenaline, and phase II adenosine diphosphate, with IC50 values of 2.8, 6.6, 13.3, 18.6, and 11.8 μM, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pirrinone (2.0 mg/kg; p.o.; single administration) enhances left ventricular contractility, increases heart rate, and transiently reduces blood pressure in conscious dogs[1].
Pelnirone (0.25-5.00 mg/kg; intravenous injection; single bolus) dose-dependently inhibits white thrombus formation in a rabbit arteriovenous shunt model, with an inhibition rate of 76.7% at the highest tested dose of 5.00 mg/kg i.v[2].
Pirfenidone (0.625-2.5 mg/kg; intravenous injection; 10% bolus, 90% continuous infusion for 4.5 h) exerts antithrombotic activity in a canine coronary thrombosis model, inhibits epinephrine-sensitized platelet aggregation, and produces dose-dependent hemodynamic effects, including hypotension, tachycardia, and increased myocardial contractility[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Unselected breed/sex, 10-20 kg (pentobarbital-induced congestive heart failure)[1]
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Dosage:0.01-1.0 mg/kg (i.v.); 0.2 mg/kg (i.d.)
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Administration:i.v. (every 30 minutes, non-cumulative); i.d. (single dose)
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Result:Achieved an ED50 of 0.03 mg/kg for increasing peak positive dP/dt by 50% and an ED20 of 0.12 mg/kg for reducing mean arterial blood pressure by 20% via intravenous administration, resulting in an ED20/ED50 ratio of 4.
Produced a dose-related increase in myocardial contractility (dP/dt max) from 11% to 222% relative to failed control via intravenous doses of 0.01-1.0 mg/kg.
Produced a dose-related increase in heart rate from 4% to 52% relative to failed control via intravenous doses of 0.01-1.0 mg/kg.
Produced a dose-related reduction in mean aortic blood pressure from 0 to 38% relative to failed control via intravenous doses of 0.01-1.0 mg/kg.
Achieved an ED50 of 0.2 mg/kg for increased dP/dt and an ED20 of >3 mg/kg for blood pressure reduction via intraduodenal administration, resulting in an ED20/ED50 ratio of >15.
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Animal Model:Unselected breed/sex, with chronically implanted Konigsberg left ventricular pressure transducers[1]
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Dosage:2.0 mg/kg
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Administration:p.o. (single dose; monitored for 6 hours)
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Result:Showed a slightly more rapid onset of action and longer duration of action compared to milrinone and compound 49.
Increased heart rate and decreased mean blood pressure that lasted during the first 2.5 hours post-dosing.
Increased left ventricular dP/dt.
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Animal Model:New Zealand rabbits (male, 2.0-2.5 kg)[2]
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Dosage:0.25 mg/kg; 0.50 mg/kg; 1.00 mg/kg; 5.00 mg/kg
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Administration:i.v.; single bolus
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Result:Reduced white thrombus formation (platelet accretion) by 7.3% at 0.25 mg/kg.
Reduced white thrombus formation (platelet accretion) by 41.7% at 0.50 mg/kg.
Reduced white thrombus formation (platelet accretion) by 56.8% at 1.00 mg/kg.
Reduced white thrombus formation (platelet accretion) by 76.7% at 5.00 mg/kg.
Chemical Information
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No. CAS 94386-65-9
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Peso molecular 241.25
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Fòrmula C12H11N5O
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SMILES
N#CC=1C(=O)N=C(NC1NCC=2C=NC=CC2)C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Bagli J, et al. Chemistry and positive inotropic effect of pelrinone and related derivatives. A novel class of 2-methylpyrimidones as inotropic agents. J Med Chem. 1988 Apr;31(4):814-23. [Content Brief]
[2]. Patelunas DM, et al. Comparative antithrombotic activities of the phosphodiesterase inhibitors pelrinone (AY-26,768), AY-31,390 and milrinone. Thromb Res. 1991;62(5):389-400. [Content Brief]
[3]. Kitzen JM, et al. Antithrombotic activity of the phosphodiesterase III inhibitor pelrinone in a canine model of coronary artery thrombosis: enhancement of efficacy with concurrent alpha 2-adrenergic antagonism. J Cardiovasc Pharmacol. 1991;18(6):777-790. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pelrinone Related Classifications
HY-106830 Related Classifications
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