论文部分内容阅读
Nilutamide(Anandron)是一种新的非甾体抗雄激素药。合成将3-三氟甲基-4-硝基苯异氰酸(Ⅰ)与2-氨基-2-氰基丙烷(Ⅱ)缩合,经减压浓缩及硅胶层析(二氯甲烷:丁酮=8:2 V/V洗脱),得中间体Ⅲ;然后将Ⅲ加入盐酸水溶液中,加热、冷却后倒入水中,沉淀物经过滤、洗涤和干燥,即得本品[FR 7533084]。药理作用本品能与雄激素受体结合,但对其他甾体激素受体无结合效应,故没有激素副作用。对大鼠睾丸微粒体17-羟化酶活性具有轻度竞争性抑制作用。大鼠阉割后,本品能抑制前列腺摄入睾丸酮,完全拮抗雄激素对前列腺及精囊生长发育的影响。大鼠口服有效剂量为10 mg/kg,经1小时吸收,达血药峰值,持续约6小时,消除半
Nilutamide (Anandron) is a new non-steroidal anti-androgen drug. Synthesis 3-Trifluoromethyl-4-nitrobenzene isocyanates (I) were condensed with 2-amino-2-cyanopropane (II), concentrated under reduced pressure and chromatographed on silica gel = 8: 2 V / V) to afford intermediate III; then III is added to aqueous hydrochloric acid, heated, cooled and poured into water, the precipitate is filtered, washed and dried to give the product [FR 7533084]. Pharmacological effects This product can combine with androgen receptor, but no other steroid hormone receptor binding effect, so there is no hormonal side effects. Slightly competitive inhibition of 17-hydroxylase activity in rat testis microsomes. After castration in rats, this product can inhibit the prostate intake of testosterone, completely antagonize the effects of androgens on prostate and seminal vesicle growth and development. Oral effective dose of 10 mg / kg, absorbed by 1 hour, peak blood levels, lasted about 6 hours, eliminating half