Proparacaine
Based on 3 publication(s) in Google Scholar
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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- CAS No.: 499-67-2
- 화학식: C16H26N2O3
- 분자량:294.40
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) Proparacaine
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Biological Activity
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.
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, 205-255 g)[3]
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Dosage:0.20, 0.44, 0.59, 1.17, and 2.92 μmol/kg
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Administration:s.c.; single injection; i.p. (single injection, no effect)
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 499-67-2
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분자량 294.40
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화학식 C16H26N2O3
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SMILES
O=C(OCCN(CC)CC)C1=CC=C(OCCC)C(N)=C1
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Synonyms
Proxymetacaine
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (3)
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Journal Impact Factor
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Most Recent
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Nat Biomed Eng
A live bacteria enzyme assay for identification of human disease mutations and drug screening. [Abstract]2025 Sep;9(9):1547-1556. PMID: 40307426 -
Mol Ther Nucleic Acids
2026 Jun 16;37(2). PMID: 42239495 -
FASEB J
Long non-coding RNA SNHG11 regulates the Wnt/β-catenin signaling pathway through rho/ROCK in trabecular meshwork cells. [Abstract]2023 Apr;37(4):e22873. PMID: 36929360
순도&문서
References
[1]. Çalışkan B, et al. The effect of brimonidine and proparacaine on metabolic enzymes: Glucose-6-phosphate dehydrogenase, 6-phosphogluconate dehydrogenase, and glutathione reductase. Biotechnol Appl Biochem. 2022;69(1):281-288. [Content Brief]
[2]. Dang A, et al. An Analysis of the Use of Proparacaine in Cataract Surgery. Cureus. 2022;14(2):e22175. Published 2022 Feb 13. [Content Brief]
[3]. Chen YW, et al. Adding Dopamine to Proxymetacaine or Oxybuprocaine Solutions Potentiates and Prolongs the Cutaneous Antinociception in Rats. Anesth Analg. 2018;126(5):1721-1728. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Proparacaine Related Classifications
HY-66012A Related Classifications
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