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.
For research use only. We do not sell to patients.
- CAS No.: 140-65-8
- Formula: C17H27NO3
- Molecular Weight:293.40
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
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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CAS No. 140-65-8
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Molecular Weight 293.40
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Formula C17H27NO3
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SMILES
CCCCOC(C=C1)=CC=C1OCCCN2CCOCC2
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Synonyms
Pramoxine
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cardiac voltage-sensitive optical mapping
Cardiac voltage-sensitive optical mapping records changes in transmembrane potential from cardiac tissue by staining the preparation with a voltage-sensitive dye and imaging fluorescence changes during electrical activation; the resulting optical action potentials can be used to map activation time, action potential duration, conduction velocity, wavefront propagation, and arrhythmia dynamics. The optical signal represents a relative fluorescence change from a tissue volume rather than a single-cell intracellular recording, so spatial resolution, sampling rate, voltage resolution, optical magnification, light penetration, and motion control must be considered together when interpreting optical action potentials.
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Neuronal voltage-sensitive dye imaging
Neuronal voltage-sensitive dye imaging detects membrane-potential-dependent optical changes from dyes associated with neuronal membranes, enabling optical recording of electrical activity from single neurons, dendrites, axons, spines, or neuronal populations in brain slices and cultured neurons. VSD signals are typically reported as fractional fluorescence or absorbance changes over baseline, such as ΔF/F or ΔI/I, and published protocols use high-speed cameras or photodiode arrays because neuronal voltage signals occur on millisecond time scales. Fast VSD imaging can be applied at two common scales: bulk staining of brain slices to measure circuit-level spatiotemporal activity, and single-cell loading or biolistic delivery to record membrane-potential transients from individual neuronal compartments. Optical signals should be interpreted as membrane-potential-related readouts, and validation by simultaneous electrophysiology or pharmacological controls is recommended when the experimen
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Acute brain-slice whole-cell patch-clamp recording
Acute brain-slice whole-cell patch-clamp recording measures membrane voltage or ionic current from visually targeted cells in living brain slices; after giga-seal formation, the membrane under the pipette is ruptured to provide low-resistance electrical access to the cell interior, enabling current-clamp analysis of excitability and voltage-clamp analysis of synaptic or membrane currents. Acute slices preserve local tissue architecture better than dissociated preparations and allow visually guided recording from defined brain regions or fluorescently labeled cells; however, whole-cell access also permits exchange between pipette solution and cytoplasm, so intracellular dialysis must be considered when interpreting signaling-dependent phenomena.
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TPA/Croton Oil Ear Edema and Dermatitis
The TPA (12-O-tetradecanoylphorbol-13-acetate) and croton oil-induced mouse ear edema model is a well-established acute cutaneous inflammation system used to evaluate topical anti-inflammatory activity by measuring edema formation, neutrophil infiltration, vascular permeability, and cytokine-mediated skin responses in vivo. The inflammatory response is triggered by topical application of phorbol esters (TPA) or croton oil constituents, leading to rapid activation of protein kinase C signaling, leukocyte recruitment, and increased vascular permeability, which can be quantified by ear thickness, weight, dye extravasation, and biochemical markers such as myeloperoxidase (MPO) activity and pro-inflammatory mediators in ear tissue homogenates. This model is widely used for screening anti-inflammatory agents, where reductions in edema and inflammatory biomarkers reflect suppression of acute dermal inflammation and immune cell infiltration. Histological evaluation typically confirms epidermal
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Transepithelial/transendothelial electrical resistance assay
TEER measures electrical resistance across epithelial or endothelial monolayers cultured on permeable supports, and the readout reflects ionic conductance through the cell barrier, especially the paracellular pathway regulated by junctional integrity. TEER can be measured without destroying the monolayer and is commonly used before or during transport, permeability, barrier-disruption, and barrier-maturation experiments. TEER values are influenced by biological maturation and technical conditions; reported factors include temperature, medium formulation, passage number, electrode geometry, membrane properties, and junctional length during early monolayer maturation. Therefore, TEER should be interpreted with blank-insert subtraction, area normalization, repeated readings, and, when possible, orthogonal barrier readouts such as FITC-dextran flux or tight-junction staining.
Purity & Documentation
References
[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)