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

Proparacaine (Proxymetacaine) 是一种局部麻醉剂。Proparacaine 可阻断神经元细胞膜上的电压门控钠离子 (Sodium Channel) 通道，从而阻止信号传导和痛觉信号传递。Proparacaine 可阻断眼部的痛觉信号，还能诱导眼肌松弛，以减少手术过程中的眼球活动。Proparacaine 可用于白内障的相关研究。

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Proparacaine

Proparacaine Chemical Structure

CAS No. : 499-67-2

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Proparacaine 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

Proparacaine 可竞争性抑制从人红细胞中纯化得到的6-磷酸葡萄糖酸脱氢酶 (6PGD) 的活性，其 IC50 为 601.60 μM，Ki 为 811.50 μM[1]。
Proparacaine 可非竞争性抑制从人红细胞中纯化得到的谷胱甘肽还原酶 (GR) 的活性，其 IC50 为 686.90 μM，Ki 为 1,654.00 μM[1]。
Proparacaine 可改变角膜上皮的肌动蛋白细胞骨架[2]。

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

Proparacaine 相关抗体:
体内研究
(In Vivo)

Proparacaine (0.20-2.92 μmol/kg；皮下注射；单次给药) 可在大鼠中诱导剂量依赖性的皮肤镇痛作用，其 ED50 为 0.57 μmol/kg；与 Dopamine (HY-B0451) 联合给药可产生协同镇痛效应，增强镇痛的强度和持续时间[3]。

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: 0.20-2.92 μmol/kg; 0.57 μmol/kg (ED50); 0.285 μmol/kg (1/2 ED50, coadministered with dopamine 1/2 ED50); 14.0 μmol/kg (combination ED50)
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.
分子量

294.40

Formula

C16H26N2O3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Proparacaine 相关分类

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  • 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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