2. Membrane Transporter/Ion Channel
  3. Sodium Channel
  4. Proparacaine

Proparacaine (Proxymetacaine) is a local anesthetic. Proparacaine blocks voltage-gated sodium channels on neuronal cell membranes, thereby inhibiting signal conduction and nociceptive signal transmission. Proparacaine blocks nociceptive signals in the eye and induces ocular muscle relaxation to reduce eye movement during surgery. Proparacaine is used in research related to cataracts.

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Proparacaine

Proparacaine Chemical Structure

CAS No. : 499-67-2

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Proparacaine Related Antibodies

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Description

Proparacaine (Proxymetacaine) is a local anesthetic. Proparacaine blocks voltage-gated sodium channels on neuronal cell membranes, thereby inhibiting signal conduction and nociceptive signal transmission. Proparacaine blocks nociceptive signals in the eye and induces ocular muscle relaxation to reduce eye movement during surgery. Proparacaine is used in research related to cataracts[1][2][3].

In Vitro

Proparacaine competitively inhibits the activity of 6-phosphogluconate dehydrogenase (6PGD) purified from human erythrocytes, with an IC50 of 601.60 μM and a Ki of 811.50 μM[1].
Proparacaine non-competitively inhibits the activity of glutathione reductase (GR) purified from human erythrocytes, with an IC50 of 686.90 μM and a Ki of 1,654.00 μM[1].
Proparacaine alters the actin cytoskeleton of corneal epithelial cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Proparacaine Related Antibodies
In Vivo

Proparacaine (0.20-2.92 μmol/kg; s.c.; single injection) induces dose-dependent cutaneous antinociception in rats with an ED50 of 0.57 μmol/kg, and coadministration with Dopamine (HY-B0451) produces a synergistic antinociceptive effect that enhances both the magnitude and duration of block[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley (male, 205-255 g)[3]
Dosage: 0.20, 0.44, 0.59, 1.17, and 2.92 μmol/kg
Administration: s.c.; single injection; i.p. (single injection, no effect)
Result: Produced dose-dependent cutaneous antinociception.
Induced 46% maximal possible effect (% MPE) of nociceptive block at ED50 dose.
Induced 100% MPE (complete nociceptive block in all 8 rats) when coadministered at 1/2 ED50 with dopamine 1/2 ED50.
Showed synergistic antinociceptive interaction with dopamine via isobolographic analysis: experimental ED50 of the combination (14.0 μmol/kg, 95% CI 12.5-15.6) was significantly lower than theoretical additive ED50.
Produced no cutaneous antinociceptive effects when administered i.p. at 2.92 μmol/kg alone or coadministered with dopamine at 1/2 ED50.
Clinical Trial
Molecular Weight

294.40

Formula

C16H26N2O3
CAS No.
SMILES

O=C(OCCN(CC)CC)C1=CC=C(OCCC)C(N)=C1
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Proparacaine Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Proparacaine499-67-2ProxymetacaineSodium ChannelNa channelsNa+ channelsspinal blockcutaneous trunci muscle reflex6PGDvoltage-gated sodium channelseyeneuronal membranescorneal epitheliumGRhuman erythrocytesactin cytoskeletonInhibitorinhibitorinhibit

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