Biological Effects of 17α-Ethynyl-4-Estrene-3β, 17β-Diol-Diacetate

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Abstract
Biological activities of 17α-ethyny1-4-estrene-3β, 17β-diol diacetate (EEDDA) were investigated in comparison with those of 17α-ethynyl-19-nortestosterone (ENT), 17α-methy1-19-nortestosterone (MNT), 17α-ethynyl-5 (10) -estrene-17β-ol-3-one (EEO) and 17α-ethynyl-4-estrene-17β-ol (EEL).Subcutaneous administration of EEDDA produced progestational activity in the McPhail assay and the endometrial carbonic anhydrase test. But the dose-response curves of EEDDA in these assays were characteristic. The maximal response was obtained in a total dose of 500-1000μg, and as the dose was increased above 1000μg, the responses of endometrium were reversed. No such reversal was obtained following treatment with progesterone and other estrogenic progestins at the dose-range in this experience.Administration of EEDDA produced a marked increase in the weights of uteri in immature mice. Since this effect was similar to those of the above-mentioned steroids, EEDDA should belong in the category of estrogenic progestin. In Allen-Doisy test, estrual changes in the vaginal smears were observed in the dose of 0.1mg.The slope of dose-response-curve obtained with EEDDA, as well as with other estrogenic progestins, in uterotrophic activity was shallow and was of the impeded type. These results might be due to their inherent antiestrogenic activities.Slight androgenic-myotrophic activity was observed after EEDDA administration in castrated male rats.Anti-inflammatory and thymolytic activities were not manifested by EEDDA treatment in adrenalectomized immature male rats.Long term administration of EEDDA resulted marked inhibition in rat hypothalamo-hypophyseo-gonadal axis, but no suppression in the adrenal weight.Studies on the metabolism of EEDDA in rat revealed that this was partly converted to 17α-ethynyl-4-estrene-3β, 17β-diol in the small intestin and to ENT in the liver. It was suggested that this conversion was responsible for the resemblance of biological activities between EEDDA and ENT.

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