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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Membrane Transporter & Ion Channel > BenzocaineCAS：1994/9/7
Molecular Formula：C9H11NO2
Molecular Weight：165.19
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to light yellow Solid
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| CAS | 1994/9/7 |
| Name | Benzocaine |
| Molecular Formula | C9H11NO2 |
| Molecular Weight | 165.19 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to light yellow Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 202-303-5 |
| MDL | MFCD00007892 |
| SMILES | CCOC(=O)C1=CC=C(C=C1)N |
| InChIKey | BLFLLBZGZJTVJG-UHFFFAOYSA-N |
| InChI | InChI=1S/C9H11NO2/c1-2-12-9(11)7-3-5-8(10)6-4-7/h3-6H,2,10H2,1H3 |
| PubChem CID | 2337 |
| Target Point | Sodium Channel |
| Passage | Membrane Transporter&Ion Channel |
| Background | Benzocaine, the active ingredient in many over-the-counter anesthetic creams, such as mouth ulcer products, works by reversibly inactivating voltage-dependent sodium channels. |
| Biological Activity | Benzocaine 与所有其它局部麻醉药 (LAs) 一起，作用电压门控Na+通道的共同受体，其在 +30 mV 下测得的 IC50 值为0.8 mM。[1-3] |
| IC50 | 0.8mM(Na+ channel)[1]. |
| In Vitro | 苯佐卡因以剂量依赖性方式阻断μ1野生型Na +电流。当施加+ 30mV的测试电位时，估计抑制50％Na +电流的苯佐卡因浓度(IC50)为约0.8mM。苯并卡因(从6.6到9.9 mV)也显著降低了h∞曲线的斜率。 μ1-N1584A的突变也显著增加了苯佐卡因的效力。在1mM时，苯佐卡因阻断约55％的野生型Na +电流但约95％的μ1-N1584A突变电流。与野生型相比，苯佐卡因似乎与N1584A突变体中的LA受体结合更强[1]。 Caz +摄取的抑制发生在较低的苯佐卡因浓度(IC50 = 40.3±1.2mM)，而不是影响酶活性[2]。 |
| In Vivo | 一种常见的含苯佐卡因麻醉剂局部应用于以下物种：狗，家养短毛猫，Long-Evans大鼠，Sprague-Dawley大鼠，雪貂，恒河猴，食蟹猴，猫头鹰猴，新西兰白兔，小型猪，ICR小鼠，C3H小鼠和C57BL / 10SnJ小鼠。除小鼠和大鼠外，所有动物均接受2秒喷雾至鼻咽粘膜，估计剂量为56mg。对啮齿动物的口腔粘膜进行2秒喷雾可为这些动物提供过大量的液体。几个月后在狗中重复该研究以确认低反应。在大多数测试的动物中观察到对苯佐卡因喷雾的反应，在给药后15至30分钟内反应达到峰值[3]。 |
| Data Literature Source | [1]. Wang GK et al. A common local anesthetic receptor for benzocaine and etidocaine in voltage-gated mu1 Na+ channels. Pflugers Arch. 1998 Jan;435(2):293-302. [2]. Di Croce D et al. Drug action of benzocaine on the sarcoplasmic reticulum Ca-ATPase from fast-twitch skeletal muscle. Naunyn Schmiedebergs Arch Pharmacol. 2015 Nov;388(11):1163-70. [3]. Davis JA，et al. Benzocaine-induced methemoglobinemia attributed to topical application of the anesthetic in several laboratory animal species. Am J Vet Res. 1993 Aug;54(8):1322-6 |
| Unit | Bottle |
| Specification | 500mg 1g |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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