Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: DrugBank:APRD00691 (EE2)
 7,802 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Uteroglobin was obtained from 5 day pregnant rabbits and purified to homogeneity by Sephadex G 75 and DEAE-cellulose chromatographies. Progesterone binding to uteroglobin was decreased by lyophilization and enhanced by SH-reducing agents. Dithiothreitol was more effective than dithioerythritol, and beta-mercaptoethanol was only active at 25 to 100 mM concentrations. SH-blocking agents (iodoacetate, iodoacetamide, phydroxymercuribenzoate and, dithiobisnitrobenzoic acid) inhibited binding. In the absence of SH-reducing agents only one in every 500 uteroglobin molecules bound the hormone, whereas under optimal conditions (20 mM dithiothreitol) one in every two molecules bound progesterone. There was no significant difference in equilibrium dissociation constants under these two conditions. Uteroglobin had a relatively high affinity for progesterone (KD=4.1 X 10(-7)M) but a threefold higher affinity for 5alpha-pregnane-3,20-dione (KD=1.3 X 10(-7)M). Estradiol was bound but non-specifically with a very low affinity, and its binding was not enhanced by SH-reducing agents. Hormonal specificity of binding to uteroglobin was different from that of binding to rabbit uterine progesterone receptor. Various synthetic progestagens (chlormadinone acetate, norethisterone, R5020) were bound to the latter but not to the former protein. Diethylstilbestrol had some affinity (15% of that of progesterone) for uteroglobin and no affinity for the progesterone receptor. Uteroglobin incubated in the presence or absence of cofactors (NADH and NADPH) with or without dithiothreitol did not metabolize progesterone.
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PMID:Interaction of uteroglobin with progesterone, 5alphapregnane-3,20-dione and estrogens. 1 Oct 93

The splenomegaly assay (Simonsen, 1962) was standardized using different strains of rats and mice. Male Wistar rat (donor)-female Swiss mouse (host) was found to be the suitable combination that could be employed in subsequent experiments to study the potential of contraceptive steroids to alter CMIR. The index of splenomegaly appeared to increase in case of mice treated with combination oral contraceptives (Ovulen, Ovral or Enovid). The differences observed, however, neared significance only in the case of Ovral (0-05 less than P less than 0-1). Neither chlormadinone acetate nor megestrol acetate significantly altered the index of splenomegaly.
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PMID:Cell-mediated immune response in mice treated with steroidal contraceptives. 5 27

A multicenter randomized double-blind trial was conducted to compare 55 women using Loestrin-20 (20 ug ethinyl estradiol and 1 mg norethisterone acetate) as an oral contraceptive with a like number of women using Microgynon-30 (30 ug ethinyl estradiol and 150 ug levonorgestrel). 7 family planning clinics agreed to collaborate in the trial and enrollment of patients which began in November 1974. The number of participating clinics was increased to 12 at a later date. 133 patients were recruited between November 1974 and September 1976. 23 were excluded from the analysis. 55 of the remaining 110 patients were admitted to each of the 2 treatment groups. It was found that women who used Loestrin-20 discontinued treatment because of abnormal bleeding more frequently that women using Microgynon-30, but that the discontinuation rates for other reasons were closely similar in the 2 treatment groups. Of the 13 women who stopped using Loestrin-20 because of abnormal bleeding, 6 complained of oligomenorrhea or amenorrhea while the other 7 complained of irregular bleeding. Of the 2 women who stopped using Microgynon-30 because of bleeding problems, 1 complained that the bleeding was irregular and the other that it was prolonged. Although the sample size is small, Loestrin-20 clearly provides poor cycle control and consequently is less acceptable than Microgynon-30. Loestrin-20 may be less effective than Microgynon-30, but the difference in the accidental pregnacy rates is not statistically significant.
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PMID:A randomized double-blind trial of two low dose combined oral contraceptives. 37 92

Intact and castrated male rats were injected daily for 10 days, beginning at 35 days of age, with either oil or one of the following steroids: testosterone propionate, dihydrotestosterone benzoate, androsterone acetate, androstenedione, androstandiol, or estradiol benzoate. Doses were 200 micrograms/rat/day for all androgens and 0.5 microgram or 2 micrograms/rat/day for estradiol. Significant increments in prolactin levels (fourfold over control values) in intact and castrated males were obtained after testosterone propionate and androstenedione treatment. Dihydrotestosterone, androsterone, and androstandiol did not induce any changes in either intact or castrated rats. Estradiol-treated males showed a four- and sevenfold increment in serum prolactin with the 0.5- and 2-microgram doses, respectively. These results suggest that androgens have a role in the control of prolactin secretion, particularly those that can be aromatized to estrogens by different tissues, including the hypothalamus.
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PMID:Effect of aromatizable androgens and estradiol on prolactin secretion in prepuberal male rats. 48 35

Sequential birth control pills are less common than monophasic pills, partly because the "first generation" sequential pills, which used estrogen only during the 1st part of the cycle, were more dangerous than the monophasic pills. Nevertheless, it is necessary to compare the "2nd generation" sequential pills which use an estrogen/progesterone combination in the 1st half of the cycle. Useful measures for comparison are estrogen content in equivalent doses of mestranol (EEME) and progesterone content in equivalent does of medroxyprogesterone-acetate (MPA). The Czech product Norbiogest (Spofa), along with Stedril-d (Wyeth), Microgynon (Shering), and Rigavidon (Richter) had the lowest dose of estrogen - .05 mg./day - in both parts of the cycle. The product Tri-Ervonum (Glaxo) has potent estrogen activity at .1mg/day throughout the cycle, but it is still less than the discontinued product Antigest (Spofa), which utilized 0.17 mg. estrogen daily, and was estrogen dominant in both parts of the cycle. Norbiogest (Spofa) is estrogen dominant in the 1st half of the cycle and progesterone dominant in the 2nd half. Norbiogest (Spofa) exhibits less extreme dominance in both parts of the cycle than does its parent drug, Biogest (Spofa). If the norethesterone in Norbiogest was replaced with norethesterone-acetate in equal weights, the 1st part of the cycle would be balanced, neither estrogen nor progesterone dominant. This "Neo"-Norbiogest would be similar to Perikursal (Wyeth).
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PMID:[How to distinguish 2-phase (sequential) steroid contraceptives]. 64 1

Rat ventral prostate of adult male rats contain a large amount of prostatic binding protein (PBP). Immunological evidence indicates that this protein is a specific secretion product of this gland. The amount and concentration of PBP in ventral prostate show marked changes as a function of age. PBP is low but detectable (0.009 and 0.002 U/mg prostate) in 5- and 10-day-old rats and increases thereafter in a biphasic way to adult levels (0.619 U/mg prostate). After castration of PBP drops to 0.054 U/mg prostate after 10 days and 0.030 U/mg prostate after 21 days. The concentration of PBP returns to precastration levels after 2 weeks of androgen treatment. Estradiol and progesterone are ineffective in this respect. The antiandrogen, cyproterone acetate, counteracts the stimulatory effect of testosterone propionate.
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PMID:Secretion of prostatic binding protein by rat ventral prostate: influence of age and androgen. 74 33

The in vitro nucleoside incorporation and methylation of uterine RNA was examined by incubating immature rat uteri with either 3H-uridine, 3H-uridine-3H-cytidine, and/or 14C-methyl-methionine. Radioactivity was determined in extracted RNA which was fractionated by gel electrophoresis or by differential solubility in zine acetate or lithium chloride. Estradiol (E2)-treated uteri respond by showing a maximum in vitro incorporation of nucleosides into total RNA and high M.W. RNA within one hr of in vivo treatment. Nucleoside incorporation into low M.W. RNA increased gradually throughout the first 3 hrs of a 4-hr hormone treatment period. E2 in vivo also caused increased in vitro methylation of total, high, and low M.W. uterine RNA fractions. Methylation of all fractions increased through the first 3 hrs of hormone treatment, but greater methylation of low M.W. RNA was apparent. The data indicate that in vivo E2 treatment stimulates an initial transitory stage of in vitro nucleoside incorporation into uterine RNA followed by a more prolonged interval of RNA methylation.
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PMID:Effects of estradiol on in vitro nucleoside incorporation and methylation of rat uterine ribonucleic acid. 92 51

Plasma hormone quantification by means of competitive protein binding or radioimmunoassay used in studying ovarian steroids is reported. Estradiol (E2) and 17 hydroxyprogesterone (17 OH-P ) plasma concentrations are indexes in the prediction of ovulation. Values of E2 in anovulatory and ovulatory cycles were significantly different (P less than .05). However, because of the sensitivity of the current methods, 17 OH-P is more reliable in predicting ovulation. A single plasma proge sterone (P) measurement made 72 hours after the elevation in basal body temperature, of greater than 5.7 ng/ml, was sufficient for assessing indirectly the occurrence of ovulation. 17 OH-P levels were found to be 8-10 times higher in a group of patients with polycystic ovaries as compared with normal women. Luteinizing hormone (LH) was significantly suppressed while follicle stimulating hormone levels remained unaffected when parametasone acetate (6 mg/day for 5 days) was given to both groups to suppress the adrenal source. It is suggested that LH release at the hypothalamic level is effected by corticosteroids. The E2/testosterone (T) ratio was also evaluated in women with polycystic ovaries given clom iphene citrate to induce ovulation. Ovulation was induced when the E2/T ratio was greater than .07. However, in the instance of T concentration greater than 1.0 ng/ml, there could be a negative response. The peripheral estrogen levels in some "estrogen-dependent" diseases suggest the description "hyperestrogenemia" is inaccurate and better referred to as hyperestrogenic tissue concentrations.
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PMID:Clinical and functional correlation of plasma steroids--diagnostic uses. 110

The estrogen potencies of 9 oral contraceptive pills, Enovid-E, Enovid-5, Ovulen, Demulen, Norinyl+80, Norinyl+50, Ovral, Norlestrin 1 mg. and Norlestrin 2.5 mg., were determined by bioassay. Relative estrogen potency was determined by analysis of variance. Enovid-5, the most estrogenic compound, had a potency of 4.88 compared to ethinyl estradiol, 50 mcg. equal 1.00; Ovral, the least estrogenic compound, had a potency of 0.81, a sixfold difference. Estrogen potencies at a fractional dose of 0.00155 correlate with reports of the incidence of minor side effects and thromboembolic disease. The effect of progestins on estrogen potency was purely additive (norgestrel and norethynodrel), purely antagonistic, or additive at low concentrations and antagonistic at high concentrations (norethindrone, norethindrone acetate, and ethynodiol diacetate). These results suggest that pills with a greater margin of safety might be developed by utilizing greater ratios of progestin to estrogen. In addition, differences in relative estrogen potency of oral contraceptive pills may be used as a basis for better clinical selection.
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PMID:Estrogen potency of oral contraceptive pills. 111 20

18 women were treated with Deposition (4th, 11th, and 18th cycle day each, 1 mg 17alpha-Ethynyl-3-isopropylsulfonyloxy-Estradiol; 25th cycle day, 10 mg norethisterone acetate). When these medicines were taken, the activities of aminotransferases, alkaline phosphatase and alpha-amylase, cholesterol, total bilirubin and proteins of the serum, TTT, and indocyanine green were measured. A little significant decrease of the activity of alaninamino transferase (GPT) was to be stated. Whereas at the end of the 6th cycle the TTT as well as the contents of total proteins and albumin, showed a little significant decrease and the contents of alpha-2-globulin, beta-globulin as well as cholesterol were statistically shown to grow. The indocyanine green elimation was longer at the end of the 6th cycle without any pathological worth from the clinical point of view being proved.
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PMID:[Liver function tests after a 6-month deposiston therapy]. 118 58


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