炔诺酮肟与炔诺酮抗着床作用的比较及其对卵巢孕酮分泌的影响

A Comparison of Anti-implantation Action of Norethisterone Oxime with that of Norethisterone and Their Effects on Progesterone Secretion in Rat Ovary

本文比较了炔诺酮肟与炔诺酮对大鼠,金地鼠及家兔3种动物的抗着床作用,用放射免疫法测定了两药引起大鼠卵巢静脉血中孕酮含量的变化。结果显示:随动物种属不同,炔诺酮肟的抗着床作用比母体炔诺酮强2～10倍。最小100％抗着床剂量的炔诺酮肟能抑制大鼠卵巢分泌孕酮,其作用比同等剂量的炔诺酮明显增强。提示炔诺酮A环三位酮基肟化能提高炔诺酮的抗着床作用,并增强其对卵巢孕酮生物合成的抑制。

The anti-implantation action of norethisterone oxime (NETO) and that of norethisterone (NET) were compared in rat, hamster and rabbit. In addition, the progesterone concentrations in the ovarian vein of pseudo-pregnant rats receiving NETO or NET were measured by radioimmunoassay. The results indicate that the anti-implantation action of NETO varies with animal species. It is 2-10 times the potency of NET'S. NETO in a dosage schedule which is minimal to cause the implantation inhibition in 100% of tested animals depresses the progesterone secretion in the rat ovary. The inhibition sction of NETO is also stronger than that of NET. The results suggest that oximation of ketone group of NET at C3 is able to enhance the anti-implantation action and the suppressive effect on the biosynthesis of progesterone in the rat ovary.