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The pharmacological activity of a new prostaglandin analog 13 dehydro omega ethyl prostaglandin f 2 alpha

, : The pharmacological activity of a new prostaglandin analog 13 dehydro omega ethyl prostaglandin f 2 alpha. Acta Zoologica Sinica 24(4): 314-321

The pharmacological activity of prostaglandin F2.alpha. (DEH), a new prostaglandin [PG] analog synthesized by the Prostaglandin Research Collaborating Group of Shanghai was studied. DEH exerted a significant antifertility effect in mice when given twice a day s.c. on Day 4 and Day 5. The ED50 of antifertility action of DEH was 0.029 mg/kg. Under similar experimental conditions, the ED50 of its parent compound PGF2.alpha. was 0.36 mg/kg, which was about 12.4 times higher than that of DEH. DEH was active orally as an antifertility agent in the mice, although the doses required were relatively larger than those given s.c. Concomitant administration of Megestrol acetate (1 mg/mouse, daily), a potent progestational compound, protected pregnancy. In ovariectomized mice, administration of Megestrol acetate also maintained pregnancy. When DEH was given in addition, it failed to cause fetal resorption, which was found in intact mice treated with DEH alone. Thus the effects of DEH on pregnancy in mice appeared to be mediated through the inhibition of progesterone secretion, rather than the direct antagonistic effect to progesterone. Injection of DEH to pseudopregnant mice caused a marked reduction in weight of the traumatized uterine horn when compared with untreated controls. When Megestrol acetate was given simultaneously with DEH, the uterine weight was not different from the control. DEH given singly or in combination failed to affect the weight of the non-traumatized uterine horn. In addition, DEH also shortened the diestrus period of pseudopregnant mice, as did its parent compound PGF2.alpha. All the effects observed in this study could be explained by its luteolytic property. A marked difference in sensitivity to the antifertility effects of DEH was observed at different stages of pregnancy. During the early stage when eggs were passing through the Fallopian tube, the pregnant mice were much less sensitive. This was evidenced by the fact that the dosage of DEH required to terminate pregnancy on Day 1 and Day 2 was about 10-fold higher than that required on Day 4 and Day 5. It appeared that Day 12 and Day 13 were the least sensitive period to the antifertility effects of DEH. The reason for this difference is not yet completely known. DEH and PGF2.alpha. were examined for their activity on smooth muscles of the isolated rat uterus and stomach fundus, and rabbit jejunum. DEH was about 10-fold less potent than PGF2.alpha. on all these preparations. Like its parent PGF2.alpha., DEH had also a pressor effect on anesthetized rats, but it was only about 19.3% as effective as PGF2.alpha. The higher luteolytic potency and a lower smooth muscle activity of DEH favors its use in postconception fertility control with least gastrointestinal side effects. Evidence obtained in acute and subacute toxicity tests suggested that DEH had no apparent toxicity on experiment animals (monkeys and rats).


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