Pramocaine
Pramocaine (Pramoxine) is a topical surface anesthetic and antipruritic agent. Pramocaine reversibly inhibits voltage-gated sodium channel, reduces transmembrane permeability of sodium ions, stabilizes cell membranes, prevents depolarization, blocks action potential conduction, and inhibits peripheral slow C-fiber pathways associated with pain, pruritus and thermoception. Pramocaine can be used in research related to chronic pruritus, renal pruritus, atopic dermatitis, xerotic pruritus, uremic pruritus, and cutaneous hyperalgesia/pain.
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- No. CAS: 140-65-8
- Fòrmula: C17H27NO3
- Peso molecular:293.40
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Vero C1008 | IC50 |
>2.0 × 105M
Compound: COVC-1751585428
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Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
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10.6019/CHEMBL4651402 |
In Vivo
Pramocaine (12-120 μmol; s.c.) elicits dose-related cutaneous antinociception in male Sprague-Dawley rats, with an ED50 of 42.1 μmol[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 298 to 348 g)[2]
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Dosage:7.74 μmol/kg; 15.48 μmol/kg; 23.22 μmol/kg; 30.96 μmol/kg
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Administration:intrathecal; single injection
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Result:Elicited dose-dependent spinal block of nociception, proprioception, and motor function.
Determined ED50 values of 15.47 μmol/kg for nociceptive block, 16.46 μmol/kg for proprioceptive block, and 17.77 μmol/kg for motor block.
Reported mean ED75 and ED25 values across all three block types as 20.83 μmol/kg and 13.17 μmol/kg, respectively.
Produced 100% maximum possible effect (%MPE) for all three block types at 30.96 μmol/kg, with complete blockade times of 36.9 minutes for nociception, 17.8 minutes for proprioception, and 15.4 minutes for motor function.
Recorded full recovery times of 94.2 minutes for nociception, 65.6 minutes for proprioception, and 41.3 minutes for motor function at 30.96 μmol/kg.
Measured AUC values of 6425 (%MPE × min) for nociception, 3709 (%MPE × min) for proprioception, and 2362 (%MPE × min) for motor function at 30.96 μmol/kg.
Showed no significant difference in spinal block duration compared to bupivacaine at equipotent doses (ED75, ED50, ED25).
Chemical Information
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No. CAS 140-65-8
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Peso molecular 293.40
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Fòrmula C17H27NO3
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SMILES
CCCCOC(C=C1)=CC=C1OCCCN2CCOCC2
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Synonyms
Pramoxine
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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].
Agarwal A, et al. Topical Pramoxine in Chronic Pruritus: Where do We Stand? Indian J Dermatol. 2021 Sep-Oct;66(5):576.
[Content Brief]
[2]. Chou AK, et al. Intrathecal pramoxine causes long-lasting spinal sensory and motor block in rats. The Journal of pharmacy and pharmacology. 2018 Apr;70(4):543-549. [Content Brief]
[3]. Chou AK, et al. Skin nociceptive block with pramoxine delivery by subcutaneous injection in rats. Pharmacological reports : PR. 2018 Dec;70(6):1180-1184. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pramocaine Related Classifications
HY-167645 Related Classifications
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