Recainam
Based on 1 Customer Validation
Recainam (Wy-42362) is a potent orally active antiarrhythmic agent and a sodium channel inhibitor. Recainam elevates ventricular fibrillation threshold, suppresses induced cardiac dysrhythmias, and may accentuate cardiac tissue refractoriness heterogeneity. Recainam can be used for the research of arrhythmias.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.27%
- CAS. Nr.: 74738-24-2
- Formel: C15H25N3O
- Molecular Weight:263.38
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Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biologische Aktivität
Recainam (10-300 μM; ≥30 min) has no significant effect on key electrophysiologic variables of isolated rabbit sinoatrial node preparations, aside from modestly shortening action potential duration[2].
Recainam (10-100 μM; ≥30 min) significantly reduces the maximal rate of rise of phase 0 (V̇max) in isolated rabbit atrial muscle preparations without altering other key electrophysiologic variables[2].
Recainam (10-300 μM; ≥30 min) causes concentration-dependent reductions in the maximal rate of rise of phase 0 (V̇max) in isolated canine ventricular muscle preparations without altering action potential duration or effective refractory period[2].
Recainam (1-300 μM; ≥30 min) causes concentration-dependent reductions in the maximal rate of rise of phase 0 (V̇max), action potential amplitude, action potential duration, and effective refractory period in isolated canine Purkinje fiber preparations[2].
Recainam (10-60 μM; ≥30 min) shifts the membrane responsiveness curve in the hyperpolarizing direction in isolated canine Purkinje fiber preparations, with higher concentrations abolishing premature responses from depolarized membrane potentials[2].
Recainam (300 μM; ≥30 min) induces a frequency-dependent reduction in the maximal rate of rise of phase 0 (V̇max) in isolated canine Purkinje fiber, canine ventricular muscle, and rabbit atrial muscle preparations, and abolishes responses at frequencies >3 Hz in Purkinje fibers[2].
Recainam (100 μM; ≥10 min) depresses phase 4 depolarization and slows isoproterenol-induced automaticity in isolated canine Purkinje fiber preparations[2].
Recainam (300 μM; ≥30 min) does not affect slow channel-dependent potentials induced by high potassium and isoproterenol in isolated canine ventricular muscle and Purkinje fiber preparations[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | AUC0-∞ | T1/2 | MRT | Vss | Cmax | Bioavailability |
|---|---|---|---|---|---|---|---|---|
| Mice[3] | 54 mg/kg | p.o. | / | / | / | / | 6.4 μg/mL | / |
| Mice[3] | 120 mg/kg | p.o. | 26.9 μg·h/mL | 1.2 h | / | / | 23.5 μg/mL | / |
| Mice[3] | 208 mg/kg | p.o. | 64.3 μg·h/mL | 1.0 h | / | / | 48.7 μg/mL | / |
| Mice[3] | 100 mg/kg | p.o. | 16.6 μg·h/mL | 0.8 h | / | / | 13.5 μg/mL | / |
| Rat[3] | 20 mg/kg | i.v. | 4.1 μg·h/mL | 0.6 h | 0.6 h | 3.2 L/kg | / | / |
| Rat[3] | 100 mg/kg | p.o. | 10.5 μg·h/mL | 3.1 h | / | / | 1.3 μg/mL | 51 % |
| Rat[3] | 110 mg/kg | p.o. | 19.9 μg·h/mL | 4.5 h | / | / | 6.6 μg/mL | / |
| Rat[3] | 500 mg/kg | p.o. | 73.9 μg·h/mL | 3.6 h | / | / | 7.8 μg/mL | / |
| Rabbit[3] | 25 mg/kg | i.v. | 5.0 μg·h/mL | 0.6 h | 0.7 h | 3.6 L/kg | / | / |
| Rabbit[3] | 50 mg/kg | p.o. | / | / | / | / | 4.1 μg/mL | / |
| Rabbit[3] | 100 mg/kg | p.o. | 39.6 μg·h/mL | 3.4 h | / | / | 16.0 μg/mL | / |
| Dog[3] | 15 mg/kg | i.v. | 20.9 μg·h/mL | 1.8 h | 2.3 h | 1.2 L/kg | / | / |
| Dog[3] | 15 mg/kg | p.o. | 18.1 μg·h/mL | 2.0 h | / | / | 8.5 μg/mL | 89 % |
| Rhesus monkey[3] | 15 mg/kg | i.v. | 12.8 μg·h/mL | 1.6 h | 1.9 h | 2.2 L/kg | / | / |
| Rhesus monkey[3] | 15 mg/kg | p.o. | 12.0 μg·h/mL | 1.9 h | / | / | 3.3 μg/mL | 97 % |
Recainam (p.o.; i.v.) exhibits anti-arrhythmic activity in dogs with experimentally induced cardiac arrhythmias[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mongrel dogs (male, 14-23 kg, anesthetized with sodium pentobarbital)[1]
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Dosage:3.75 mg/kg (loading) + 0.0375 mg/kg per min (maintenance); 7.5 mg/kg (loading) + 0.075 mg/kg per min (maintenance)
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Administration:i.v.; loading dose over 20 min; maintenance infusion for remainder of experiment
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Result:Increased sinus QRS duration by 11% and paced QRS duration by 14% at low dose.
Produced no significant change in ventricular effective refractory period or sinus cycle length at low dose.
Increased E50 by 42% at low dose.
Increased sinus QRS duration by 27% and paced QRS duration by 23% at high dose.
Produced no significant change in ventricular effective refractory period or sinus cycle length at high dose.
Increased E50 by 92% at high dose.
Caused changes in E50 that were significantly different from the saline group and between low and high dose groups.
Showed no statistically significant difference in percent change of sinus QRS duration between low and high dose groups.
Chemical Information
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CAS. Nr. 74738-24-2
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Appearance Solid
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Molecular Weight 263.38
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Formel C15H25N3O
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Color Off-white to light yellow
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SMILES
CC(C)NCCCNC(NC1=C(C=CC=C1C)C)=O
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Synonyms
Wy-42362
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 50 mg/mL (189.84 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (283 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Frame LH, et al. Effect of recainam on the energy required for ventricular defibrillation in dogs as assessed with implanted electrodes. J Am Coll Cardiol. 1988 Sep;12(3):746-52. [Content Brief]
[2]. Takikawa R, et al. Electrophysiologic effects of a new antiarrhythmic agent, recainam, on isolated canine and rabbit myocardial fibers. J Am Coll Cardiol. 1988 Apr;11(4):875-81. [Content Brief]
[3]. Scatina JA, et al. Species differences in the pharmacokinetics of recainam, a new anti-arrhythmic drug. Biopharm Drug Dispos. 1990 Jul;11(5):445-61. [Content Brief]
[4]. Anastasiou-Nana MI, et al. Recainam, a potent new antiarrhythmic agent: effects on complex ventricular arrhythmias. J Am Coll Cardiol. 1986 Aug;8(2):427-35. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.7968 mL | 18.9840 mL | 37.9680 mL | 94.9199 mL |
| 5 mM | 0.7594 mL | 3.7968 mL | 7.5936 mL | 18.9840 mL | |
| 10 mM | 0.3797 mL | 1.8984 mL | 3.7968 mL | 9.4920 mL | |
| 15 mM | 0.2531 mL | 1.2656 mL | 2.5312 mL | 6.3280 mL | |
| 20 mM | 0.1898 mL | 0.9492 mL | 1.8984 mL | 4.7460 mL | |
| 25 mM | 0.1519 mL | 0.7594 mL | 1.5187 mL | 3.7968 mL | |
| 30 mM | 0.1266 mL | 0.6328 mL | 1.2656 mL | 3.1640 mL | |
| 40 mM | 0.0949 mL | 0.4746 mL | 0.9492 mL | 2.3730 mL | |
| 50 mM | 0.0759 mL | 0.3797 mL | 0.7594 mL | 1.8984 mL | |
| 60 mM | 0.0633 mL | 0.3164 mL | 0.6328 mL | 1.5820 mL | |
| 80 mM | 0.0475 mL | 0.2373 mL | 0.4746 mL | 1.1865 mL | |
| 100 mM | 0.0380 mL | 0.1898 mL | 0.3797 mL | 0.9492 mL |