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Nepafenac

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Chemical Structure| 78281-72-8 同义名 : AL 6515;AHR 9434;Nevanac
CAS号 : 78281-72-8
货号 : A174101
分子式 : C15H14N2O2
纯度 : 98%
分子量 : 254.284
MDL号 : MFCD08067732
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(412.92 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
动物实验配方：

IP 2% DMSO+2% Tween80+30% PEG300+water 10 mg/mL clear

PO 0.5% CMC-Na 61 mg/mL suspension

生物活性
靶点

  • COX-1
描述 Nepafenac is a NSAID (nonsteroidal anti inflammatory drug) that is routinely used in opthamology to control pain following cataract surgery. Nepafenac exhibited only weak COX-1 inhibitory activity (IC50 = 64.3 microM). In vitro, a single topical ocular dose of nepafenac (0.1%) inhibited prostaglandin synthesis in the iris/ciliary body (85 - 95%) and the retina/choroid (55%)[3]. Nepafenac administration significantly suppresses PGE2 synthesis in the retina/choroid. Topical nepafenac administration also significantly inhibits prostaglandin (PG)-mediated blood-retinal barrier breakdown and concurrent protein extravasation into the vitreous[4]. Short term perfusion (5 min) of the corneal surface with 0.1% nepafenac resulted in sustained flux of drug across the cornea for 6h. Under identical conditions only 3.3 microM of diclofenac accumulated on the corneal endothelial side compared to 16.7 microM nepafenac[5]. An intracameral concentration of up to 1% nepafenac does not adversely affect the rabbit eye. Nepafenac fails to prevent miosis but inhibits prostaglandin release during phacoemulsification surgery[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02515045 - Completed - -
NCT02955641 Glaucoma, Closed-Angle ... 展开 >> Glaucoma, Narrow-Angle Glaucoma, Angle-Closure 收起 << Not Applicable Recruiting November 2019 Israel ... 展开 >> Sheba Medical Center Recruiting Tel HaShomer, Israel Contact: Ari Leshno       arileshno@gmail.com 收起 <<
NCT00407017 Cataract Surgery Phase 4 Completed - United States, Florida ... 展开 >> The Center for Excellence in Eye Care Miami, Florida, United States, 33176 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.93mL

0.79mL

0.39mL

19.66mL

3.93mL

1.97mL

39.33mL

7.87mL

3.93mL
参考文献

[1]Gamache DA, Graff G, et al. Nepafenac, a unique nonsteroidal prodrug with potential utility in the treatment of trauma-induced ocular inflammation: I. Assessment of anti-inflammatory efficacy. Inflammation. 2000 Aug;24(4):357-70.

[2]Gamache DA, Graff G, et al. Nepafenac, a unique nonsteroidal prodrug with potential utility in the treatment of trauma-induced ocular inflammation: I. Assessment of anti-inflammatory efficacy. Inflammation. 2000 Aug;24(4):357-70.

[3]Gamache DA, Graff G, Brady MT, Spellman JM, Yanni JM. Nepafenac, a unique nonsteroidal prodrug with potential utility in the treatment of trauma-induced ocular inflammation: I. Assessment of anti-inflammatory efficacy. Inflammation. 2000 Aug;24(4):357-70

[4]Lindstrom R, Kim T. Ocular permeation and inhibition of retinal inflammation: an examination of data and expert opinion on the clinical utility of nepafenac. Curr Med Res Opin. 2006 Feb;22(2):397-404

[5]Ke TL, Graff G, Spellman JM, Yanni JM. Nepafenac, a unique nonsteroidal prodrug with potential utility in the treatment of trauma-induced ocular inflammation: II. In vitro bioactivation and permeation of external ocular barriers. Inflammation. 2000 Aug;24(4):371-84

[6]Jha R, Sur V, Bhattacharjee A, Ghosh T, Kumar V, Konar A, Hazra S. Intracameral Use of Nepafenac: Safety and Efficacy Study. Curr Eye Res. 2018 May;43(5):630-638