Dapiprazole HCl

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Chemical Structure| 72822-13-0 同义名 : Dapiprazole (hydrochloride); Glamidolo Hydrochloride; Reversil Hydrochloride
CAS号 : 72822-13-0
货号 : A893853
分子式 : C19H28ClN5
纯度 : 99%
分子量 : 361.91
MDL号 : MFCD00941400
存储条件:

Pure form Inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Dapiprazole Hydrochloride is alpha 1-adrenoceptor antagonist. Dapiprazole produces miosis by blocking the alpha 1 receptors in the radial muscle of the iris. Intraocular 0.01% and 0.05% dapiprazole is an effective miotic agent that may be helpful during surgery when the reversal of sympathomimetic mydriasis is needed[3]. Dapiprazole, an alpha-blocking miotic drug, was used intracamerally at the end of extracapsular cataract extraction with posterior chamber intraocular lens (IOL) implantation. A significant reversal of mydriasis by intraocular dapiprazole, especially with the 0.25% and 0.5% concentrations which did not differ significantly in effectiveness and safety[4]. Comfortable reading ability returned after approximately 43 min with dapiprazole vs. 66 min without dapiprazole. All of subjects exhibited conjunctival hyperemia after the administration of dapiprazole[5]. Dapiprazole hydrochloride was perfused across endothelia in the specular microscope at concentrations from 1.25 mg/mL to 1000 mg/mL. It is evident that the drug concentration that reaches the endothelium after topical application has no toxic effect on the cornea, and that the drug should only be used as directed and not used as an anterior chamber perfusate[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.76mL

0.55mL

0.28mL

13.82mL

2.76mL

1.38mL

27.63mL

5.53mL

2.76mL

参考文献

[1]Ramesh T, Rao PN. Development and validation of a stability-indicating RP-HPLC assay method and stress degradation studies on dapiprazole. J Chromatogr Sci. 2013 Oct;51(9):856-60.

[2]Cheeks L, Chapman JM, et al. Corneal endothelial toxicity of dapiprazole hydrochloride. Lens Eye Toxic Res. 1992;9(2):79-84.

[3]Bonomi L, Marchini G, Pagello P, Simonazzi A, Durando L, Ciarniello MG. Effects of intraocular dapiprazole in the rabbit eye. J Cataract Refract Surg. 1989;15(6):681-684

[4]Ponte F, Cillino S, Faranda F, Casanova F, Cucci F. Intraocular dapiprazole for the reversal of mydriasis after extracapsular cataract extraction with intraocular lens implantation. Part I: Dose-response correlation. J Cataract Refract Surg. 1991;17(6):780-784

[5]Molinari JF, Johnson ME, Carter J. Dapiprazole clinical efficiency for counteracting tropicamide 1%. Optom Vis Sci. 1994;71(5):319-322

[6]Cheeks L, Chapman JM, Green K. Corneal endothelial toxicity of dapiprazole hydrochloride. Lens Eye Toxic Res. 1992;9(2):79-84