Sulfonyl iodides, including three previously unknown alkane derivatives, add readily and stereoselectively to acetylenes to form 1: 1 adducts in good to excellent yields. That the addition occurs in a trans manner was established by reducing the adducts to the cis-vinyl sulfones with zinc and acetic acid and by three-dimensional X-ray crystallography. The adducts represent convenient precursors to sulfonylacetylenes and, on treatment with cuprous phenylacetylide, yield the novel ene-yne sulfones. The acetylenic sulfones undergo a smooth thermally induced extrusion of sulfur dioxide in several cases.
Two patients with granulosa cell tumors of the ovary, endometrial hyperplasia, elevated serum estradiol (E2) concentrations and depressed FSH levels were studied preoperatively using intravenous administration of FSH, LH and gonadotropin-releasing hormone. In patient 1 serum E2 increased from a baseline of 72.7 to 116.8 pg/ml 60 min after hCG stimulation, with a peak level of 571.4 pg/ml 96 h after hCG administration; there was a rapid postoperative decline to 16 pg/ml. Ovarian venous E2 on the tumor side was 6,979 pg/ml. In patient 2, E2 increased from a baseline of 91 to 449 pg/ml at 20 h after FSH administration. Intraoperative ovarian venous E2 was 9,788 pg/ml. Inhibin, which was elevated in patient 1 prior to stimulation (736 fmol/ml), peaked 96 h after hCG administration. Ovarian venous inhibin concentration in patient 1 was 2,911 fmol/ml. The baseline inhibin concentration in patient 2 was not elevated (249 fmol/ml), but there was an elevation of inhibin in response to FSH administration (757 fmol/ml), but no response to hCG. Ovarian inhibin concentration was not different between the tumor and contralateral sides in patient 2. Both granulosa cell tumors were responsive to exogenous gonadotropin stimulation. Although only one tumor made significant baseline levels of inhibin, the production of inhibin by both tumors was apparently stimulated by FSH.
Metabolites of progesterone (pregnanolone and allopregnanolone) may play a physiologic role as anxiolytic agents, perhaps modifying mood and anxiety; the current study confirms the utility of twice daily, 200-mg progesterone vaginal suppositories, in the alleviation of some PMS symptoms relating to anxiety and irritability. Further evaluation may be warranted to ascertain which patients in the known heterogeneous PMS population may be most likely to benefit from such treatment.
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