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醋炔诺酮肟通过LFZ—1型旋转薄层仪分离,吸附剂采用硅胶GF_(254),以石油醚:醋酸乙酯(7:3)为溶剂系统,分别得到顺、反式异构体,重结晶后得纯品,测得其各理化参数。从H-NMR图谱分析,顺、反异构体特征吸收峰分别为δ6.54与δ5.84。醋炔诺酮肟在干燥条件下贮藏,或经C_0~(60)2.5×10~4Gy辐照,其中顺、反异构体比例不变。醋炔诺酮肟、顺、反异构体三者配成不同浓度混悬剂,经皮下注射后,比较其抑制Wistar大鼠动情周期天数,实验结果表明,小剂量时三者无区别;剂量8mg/只时,混合体与顺式异构体分别为45.7±2.6天与34.2±6.9天;16mg/时顺式为46.0±2.6天,反式为39.0±4.0天(P<0.01)。抗着床实验结果,顺式、混合体、反式的ED_(50)分别为0.53(0.40~0.64)、0.75(0.69~0.87)与0.97(0.73~1.16)mg/kg
Acetoxynil oxime was separated by LFZ-1 rotary thin-layer apparatus. Silica gel GF_ (254) was used as adsorbent and petroleum ether: ethyl acetate (7: 3) as solvent system to obtain cis and trans isomers , After recrystallization were pure, measured the physical and chemical parameters. From the H-NMR spectrum analysis, cis and trans isomers characteristic absorption peaks were δ6.54 and δ5.84. Norethindrone acetate oxime was stored under dry conditions, or by C_0 ~ (60) 2.5 × 10 ~ 4Gy irradiation, wherein cis, trans isomer ratio unchanged. Acetoxynil oxime, cis and trans isomers were dosed with different concentrations of suspension, after subcutaneous injection, compared with the inhibition of Wistar rat estrous cycle days, the experimental results show that there is no difference between the three small doses; dose At 8 mg / mouse, the mixtures and cis isomers were 45.7 ± 2.6 days and 34.2 ± 6.9 days, respectively; 46 mg ± 2.6 days at 16 mg / hr and 39.0 ± 4.0 days at trans (P <0.01). The results of anti-implantation test showed that the ED50 of cis-trans, trans-trans and trans were 0.53 (0.40-0.64), 0.75 (0.69-0.87) and 0.97 (0.73-1.16) mg / kg