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爱普列特是新一代选择性、特异性作用于甾体5(还原酶II亚型的反竞争性抑制剂(uncompetitive inhibitor)。具有抑制双氢睾丸酮生物生成及选择性抑制前列腺生长的作用。爱普列特口服吸收好,在前列腺中可保持较高浓度。口服爱普列特可导致前列腺萎缩,其作用机制主要为促进前列腺细胞凋亡,组织学可见前列腺腺腔减小及上皮细胞高度变矮,染色体凝缩率和凋亡小体发生率明显增加,凋亡抑制基因bcl-2的蛋白表达下调。药理学和毒理学研究证实爱普列特具有高度器官选择性,其主要靶器官为前列腺,而对心血管系统、呼吸系统等均未见有明显影响,生殖毒理学研究未发现明显生殖毒性,遗传毒理学研究表明无致突变作用。
Eptifibatide is a new generation of uncompetitive inhibitor of selective and specific action on steroid 5 (a reductase II subtype) that inhibits the biosynthesis of dihydrohydrotestosterone and selectively inhibits prostate growth. Epristeride oral absorption, can maintain a high concentration in the prostate oral epristeride can lead to prostate atrophy, its mechanism of action is mainly to promote apoptosis of prostate cells, histology can be seen reduced prostate gland and epithelial cell height Dwarfing, chromosome condensation rate and the incidence of apoptotic bodies increased significantly, the expression of apoptosis-inhibiting gene bcl-2 protein down.Physiology and toxicology studies have confirmed that epristeride has a high degree of organ selectivity, the main target organ For the prostate, but no obvious effects on the cardiovascular system, respiratory system, reproductive toxicology study found no significant reproductive toxicity, genotoxicity studies have shown no mutagenic effect.