Etafenone
Etafenone is an antiarrhythmic agent and vasodilator. Etafenone exerts β-adrenergic agonistic effects. Etafenone inhibits the automaticity of sinoatrial nodes, atrioventricular junctions and Purkinje fibers, prolongs action potential duration and refractory period, slows the rising rate of action potentials, and prolongs conduction time. Etafenone enhances collateral circulation after coronary occlusion and suppresses ventricular premature beats. Etafenone delays ischemic myocardial energy imbalance, improves the recovery of high-energy phosphates after ischemia, and reduces myocardial oxygen consumption. Etafenone can be used in research related to ischemic heart disease, arrhythmia and angina pectoris.
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- CAS No.: 90-54-0
- Formule: C21H27NO2
- Masse moléculaire:325.44
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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β-adrenoceptor |
Etafenone (0.5-3 mg/L) dose-dependently reduces membrane responsiveness in canine Purkinje fibers, as evidenced by a rightward shift of the membrane responsiveness curve at 0.5 mg/L and an exaggerated shift at 3 mg/L[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Cmax | Tmax |
|---|---|---|---|---|
| Dog[1] | 20 mg/kg | p.o. | 20 mg/L | 1 h |
Etafenone (0.3-3 mg/kg; i.v.) dose-dependently decreases systemic blood pressure and heart rate, increases venous return, cardiac output, and right atrial pressure at doses up to 3 mg/kg in anesthetized open-chest mongrel dogs, while higher doses above 3 mg/kg induce cardiodepressant effects with reduced venous return and cardiac output[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mongrel dogs (both sexes, 20-39 kg, starved for 24 h, anaesthetized)[3]
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Dosage:0.1 mg/kg/min; 0.5 mg/kg/min; 0.5 mg/kg/min (following propranolol pretreatment)
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Administration:i.v.; infusion over 10 min
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Result:Produced non-significant slight increases in heart rate, coronary conductance, femoral conductance, expiratory CO2, and non-significant slight decreases in arterial and left ventricular blood pressure; no change in dp/dt at 0.1 mg/kg/min.
Produced significant increases in heart rate, coronary conductance (significant only at 6-12 min), femoral conductance, left ventricular dp/dt, expiratory CO2, and myocardial oxygen consumption (significant only at 2-4 min); caused a significant fall in systemic blood pressure throughout the infusion; peak left ventricular blood pressure was unchanged; all parameters returned to preinfusion values 5-10 min post-infusion except heart rate and femoral conductance at 0.5 mg/kg/min.
Completely abolished increases in heart rate and dp/dt seen without β-blockade, with dp/dt showing a significant reduction from 10 min onwards; significant increases in coronary conductance, femoral conductance, and expiratory CO2 persisted but were significantly reduced compared to pre-β-blockade levels; systemic and left ventricular blood pressure decreased significantly throughout the infusion and remained lowered during the observation period at 0.5 mg/kg/min after propranolol pretreatment.
Chemical Information
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CAS No. 90-54-0
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Appearance Solid
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Masse moléculaire 325.44
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Formule C21H27NO2
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SMILES
O=C(C1=CC=CC=C1OCCN(CC)CC)CCC2=CC=CC=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)