Ipravacaine
Ipravacaine (IQB-9302) is a long-acting amide-based local anesthetic. Ipravacaine blocks open-state hKv1.5, with stereoselective, time-dependent and voltage-dependent inhibitory effects, and exerts stronger activity on the R (+) enantiomer. Ipravacaine blocks Kv2.1, Kv4.3 and HERG potassium channels. Ipravacaine induces negative chronotropic effects, increases mean arterial pressure, and exhibits vasodilatory effects at high concentrations.
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- No. CAS: 166181-63-1
- Fòrmula: C18H26N2O
- Peso molecular:286.41
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Help & FAQs
Actividad biológica
Descripciòn
In Vitro
Ipravacaine (10-500 μM; ~12 min) exerts stereoselective, time- and voltage-dependent open-channel block on hKv1.5 channels stably expressed in Ltk7 cells, with R (+) Ipravacaine (KD=17.8 μM) being 3.2 times more potent than S (-) Ipravacaine (KD=58.6 μM)[1].
The molecularly simulated aromatic ring-overlapping conformers of R (+) and S (-) Ipravacaine have N-substituents with opposite orientations, which explains their stereoselective blocking effect on hKv1.5 channels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (3-month-old, 250-350 g, sex-matched, anaesthetised with sodium pentobarbital)[3]
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Dosage:0.1 mg/kg; 0.3 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
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Administration:i.v.; over 30 seconds, followed by 100 μl heparinised sodium chloride infusion over 15 seconds; every 20 minutes
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Result:Produced a maximum decrease in heart rate of 114 bpm.
Produced a maximum increase in mean arterial pressure of 20.7 mmHg.
Caused all exposed rats to die within 2 minutes at 10 mg/kg, with all surviving more than 1.5 minutes post-dose.
Was well-tolerated without mortality at 3 mg/kg.
Chemical Information
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No. CAS 166181-63-1
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Peso molecular 286.41
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Fòrmula C18H26N2O
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SMILES
O=C(C1N(CC2CC2)CCCC1)NC3=C(C)C=CC=C3C
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Synonyms
IQB-9302
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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]. González T, et al. Stereoselective effects of the enantiomers of a new local anaesthetic, IQB-9302, on a human cardiac potassium channel (Kv1.5). British journal of pharmacology. 2001 Jan;132(2):385-92. [Content Brief]
[2]. Gallego-Sandin S, et al. The comparative hemodynamic effects of intravenous IQB-9302 and bupivacaine in anesthetized rats. Acta Anaesthesiol Scand. 2004 May;48(5):607-12. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Ipravacaine Related Classifications
HY-184377 Related Classifications
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