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Proparacaine Hydrochloride

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Chemical Structure| 5875-06-9 同义名 : 丙美卡因盐酸盐 ;Proxymetacaine Hydrochloride;Proparacaine HCl;Parcaine;Ophthetic;Ophthaine;Ocu-Caine;Minims;UNII-U96OL57GOY;proxymetacaine monohydrochloride;Ophthain
CAS号 : 5875-06-9
货号 : A341969
分子式 : C16H27ClN2O3
纯度 : 98+%
分子量 : 330.85
MDL号 : MFCD00083467
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(151.13 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 30 mg/mL(90.68 mM)，配合低频超声助溶
动物实验配方：

PO 0.5% CMC-Na 80 mg/mL suspension

生物活性
靶点

  • Sodium Channel

    Voltage-gated sodium channel, ED50:3.4 mM
描述 Proparacaine (PPC) Hydrochloride is a derivative of lidocaine (HY-B0185), with immunomodulatory effect and glucocorticomimetic activity. Proparacaine Hydrochloride (294.47-18.85 mM; 4-12 hours) can induce apoptosis of HCS cells. Proparacaine Hydrochloride (4.71 mM; 4-12 hours) induces G1 phase arrest, plasma membrane permeability elevation, phosphatidylserine externalization, DNA fragmentation, chromatin condensation, and apoptotic body formation of HCS cells. Proparacaine Hydrochloride (4.71 mM; 4-12 hours) downregulates and upregulates the expression of Bcl-xL and Bax, respectively, and remarkably upregulates cytoplasmic cytochrome C and apoptosis inducing factor. Proparacaine Hydrochloride (>588.93 μM; 4-28 hours) has a dose- and time-dependent cytotoxicity to HCS cells at concentrations in vitro[3]. In addition, proparacaine hydrochloride is an ester-type local anesthetic agent that is extensively used in ophthalmic operations[4]. PH (Proparacaine Hydrochloride) has a mydriatic effect of its own. It penetrates through the bare sclera and leads on to skewed dilation of the pupil[5]. 0.5% proparacaine HCl is commonly used for topical anaesthesia in ultrasound pachometry prior to refractive surgery[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.02mL

0.60mL

0.30mL

15.11mL

3.02mL

1.51mL

30.23mL

6.05mL

3.02mL
参考文献

[1]Segarra S, Papasouliotis K, et al. The in vitro effects of proxymetacaine, fluorescein, and fusidic acid on real-time PCR assays used for the diagnosis of Feline herpesvirus 1 and Chlamydophila felis infections. Vet Ophthalmol. 2011 Sep;14 Suppl 1:5-8.

[2]Grant RL, Acosta D. Comparative toxicity of tetracaine, proparacaine and cocaine evaluated with primary cultures of rabbit corneal epithelial cells. Exp Eye Res. 1994 Apr;58(4):469-78.

[3]Kim HS, Won S, Lee EK, Chun YH, Yoon JS, Kim JT, Kim HH. Effect of Proparacaine in a Mouse Model of Allergic Rhinitis. Clin Exp Otorhinolaryngol. 2017 Dec;10(4):325-331

[4]Yang Z, Zhao J, Feng Y, Lei Y, Liu D, Qin F, Zheng J, Wang S. Identification, synthesis and structural confirmation of process-related impurities in proparacaine hydrochloride. J Pharm Biomed Anal. 2020 Oct 25;190:113497

[5]Takkar B, Sharma P, Gaur N, Singh AK, Ramachandran R. Proparacaine-Induced Mydriasis During Strabismus Surgery. Semin Ophthalmol. 2018;33(3):367-370

[6]Herse P, Siu A. Short-term effects of proparacaine on human corneal thickness. Acta Ophthalmol (Copenh). 1992 Dec;70(6):740-4