Relationship between nitric oxide production and choroidal. blood flow
Relationship between nitric oxide production and choroidal. blood flow
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DOI：
10.1089/108076803321908365
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发表时间：
2003-06-01
影响因子：
2.3
通讯作者：
Peng, SX
中科院分区：
文献类型：
--
作者：
Xuan, B;Xu, XR;Peng, SX
目的：发明一种通过增加一氧化氮（NO）特异性促进脉络膜血流的药物。方法：体外实验采用细胞培养法测定NO供体的NO生成量;体内实验采用彩色微球技术测定兔眼各组织的血流量。结果：ZX-5和ZX-4为两种地理异构体，其中ZX-5为反式，ZX-4为顺式。（1-苯基-3-{3-甲氧基-2-丙氧基-5-[4-（3，4，5-三甲氧基-苯基）-1，3-二硫戊环-2-基}苯基}硫脲）。发现ZX-5在3、10、30 μ g/ml浓度下释放显著量的NO，并且在1%、50 μ l滴入眼内时增加脉络膜血流量。对虹膜、睫状体血流无明显影响。结论：ZX-5能特异性增加脉络膜血流量，对老年性黄斑变性（AMD）脉络膜新生血管的形成有抑制作用。ZX-5类化合物有望用于老年人AMD的治疗/预防。
Purpose: To invent a drug which can specifically facilitate choroid blood flow via increase of nitric oxide (NO). Method: Cell culture was used for in vitro experiments to determine the production of NO by NO donors and colored microsphere technique was used for in vivo experiments to determine the blood flow in various tissues of rabbit eyes. Results: ZX-5 and ZX-4 are two geographic isomers with ZX-5 as trans-form and ZX-4 as cis-form. (1-phenyl-3-{3-methoxy-2-propoxy-5-[4-(3,4,5-trimethoxy-phenyl)-1,3-dithiolane-2-yl{phenyl}thiourea). It was found that ZX-5 released significant amount of NO at 3, 10, 30 mug/ml concentrations and increased choroid blood flow at 1%, 50mul instillation into eyes. It was not effective on the blood flow of iris or ciliary body. The corresponding ZX-4 was not effective on ocular blood flow nor it released NO. Conclusion: ZX-5 can specifically increase the choroidal blood flow which could be useful to suppress the choroidal neovascularization in age-related macular degeneration (AMD). It is hoped that ZX-5 type of compounds could be used for the treatment/prevention of AMD in the elderly.