Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound   Target Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound

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Query: EC:2.7.10.1 (ERK)
95,504 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The estrogenic effects of MER-25, an antiestrogen, on eating and body weight were studied in rats. As evidenced by its failure to cause an habitual aversion to saccharin and failure to alter spontaneous activity, MER-25 inhibited weight gain and eating. Estradiol benzoate (EB) and MER-25 both had similar effects in gonadectomized rats, and produced a transient decrease in food consumption and a permanent decrease in body weight. Progesterone ameliorated the effect of both agents on eating and body weight. MER-25 and EB were both more active in females than males. MER-25 did not markedly alter the effects of EB on body weight and eating, but did antagonize the effects of EB on the uterus, vagina, and sex behavior. The results indicate biochemical differences between the effects of estrogens on eating and body weight and other estrogen-dependent processes.
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PMID:Estrogenic effects of an antiestrogen, MER-25, on eating and body weight in rats. 94 84

Progesterone priming of the ovariectomized rat, followed by a single injection of estradiol-17beta (10 mug) is followed by an increased uterine synthesis of both PGF and PGE. The administration of an estrogen antagonist (MER-25; 10 mg) concomitantly with estradiol had no effect on uterine prostaglandin synthesis. Similarly, the administration of either Actinomycin D or cycloheximide, antibiotics demonstrated to inhibit mRNA and protein synthesis, respectively, is without effect on estrogen-stimulated uterine prostaglandin synthesis. These results are considered with regard to the classic receptor theory of estrogen action and are a preliminary indication that estrogen-stimulated uterine prostaglandin synthesis may not require those receptor mediated events.
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PMID:Considerations into the mechanism of estrogen-stimulated uterine prostaglandin synthesis. 95 89

To assess the effect of hormonal monthly injectable contraceptives upon the serum values of immunoreactive prolactin (Prl), three groups of women of reproductive age exposed to different estrogen-progestogen injectable formulation for a minimum of one year were studied. The first group (n = 10) received dihydroxyprogesterone acetophenide 150 mg and estradiol enanthate 10 mg (DHPA/E2-EN), Group 2 (n = 21) received medroxyprogesterone acetate 25 mg and estradiol cypionate 5 mg (MPA/E2-C) and Group 3 (n = 19) was exposed to norethisterone enanthate 50 mg and estradiol valerate 5 mg (NET-EN/E2-V). A group of IUD users (n = 16) served as the control group. Serum Prl and 17 beta-estradiol (E2) concentration were determined in blood samples (0 and 15 min.) on days 0 (day of last injection), 10, 20 and 30 after last contraceptive injection. The results demonstrated a slight though not significant increase (p greater than 0.05) in serum Prl in the three experimental groups as compared with the IUD control group. This increase in Prl levels observed on day 10 post-last injection never exceeded the upper limits of the normal range (20 ng/ml). Overall, the data demonstrated that the chronic administration of these estrogen/progestogen once-a-month injectable contraceptives does not affect the Prl baseline secretion in women.
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PMID:Estrogen-progestogen once-a-month injectable contraceptives and serum prolactin. 252 62

The aim of this study was to investigate the effects of estradiol and tamoxifen (TAM) on the growth of human endometrial carcinomas in athymic mice. Tissues from primary tumors were implanted into estradiol-treated mice. In passage 2, animals were treated with (a) placebo, (b) estradiol, (c) estradiol plus TAM, and (d) TAM alone. The size of the tumors was measured weekly. Estrogen receptors (ER) were determined with the dextran-coated charcoal method and/or ER enzyme-linked immunoassay. Progesterone receptors were measured with the dextran-coated charcoal technique. Of 16 primary tumors, 2 grew in the athymic mice and were studied further. Tumor EL was positive for ER (145 fmol/mg protein) and progesterone receptors (993 fmol/mg protein). Tumor EL in passage 2 was not significantly stimulated by estradiol, but was stimulated by a combination of estradiol and TAM. Treatments (estradiol, estradiol plus TAM, or TAM) all increased tumor growth in passage 3. Tumor BR and a metastasis BR-MET were ER and progesterone receptor negative, applying dextran-coated charcoal, ER enzyme-linked immunoassay, and immunocytochemistry. The BR and BR-MET cells contain the complete ER gene but do not express any measurable amounts of ER mRNA as quantitated by Northern blot analysis, using a complete ER complementary DNA probe. In all animal passages the growth rate was significantly higher in estradiol-treated mice compared with the control. TAM alone had some growth stimulatory effect, but much smaller than observed in the estradiol group. TAM inhibited estradiol-stimulated growth. These results suggest that estradiol and possibly TAM are capable of stimulating tumor growth in the athymic mice independently from ER, potentially through a host-mediated mechanism.
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PMID:Enhanced growth of an estrogen receptor-negative endometrial adenocarcinoma by estradiol in athymic mice. 275 9

Progesterone and 5 alpha-pregnane-3,20-dione (5 alpha-DHP) were determined by radioimmunoassay in 242 amniotic fluid samples from 16-19 weeks of gestation. 165 samples fulfilled the criteria of the normal collective. There is a positive correlation (r = 0.359, p less than 0.001) between progesterone and 5 alpha-DHP. The mean concentration (+/- SD) of progesterone for normal pregnancies was 68.04 +/- 35.56 ng/ml, the mean for 5 alpha-DHP was 6.6 +/- 4.76 ng/ml. A slight decrease of the hormone concentrations with increase of the week of gestation was observed. 7 cases, who later developed EPH-gestosis showed a significant higher progesterone concentration (p less than 0.05). 16 women with premature labor had a significant higher 5 alpha-DHP concentration (p less than 0.05). Significantly elevated progesterone and 5 alpha-DHP values were found in 36 cases of bleedings in early pregnancy. Pregnant women older than 35 years proved to have a significant higher 5 alpha-DHP concentration (p less than 0.05). Also women, who delivered a child weighing less than 2,500 g (n = 8), showed a significant higher progesterone concentration (p less than 0.01). There was no difference in amniotic fluid progesterone and 5 alpha-DHP concentration depending on the sex of the child. The hormone concentrations of 3 cases with Morbus Langdon-Down were slightly below the mean concentration for progesterone and 5 alpha-DHP. Progesterone and 5 alpha-DHP concentrations were found to be normal in one case each of open Ductus Botalli, esophagial atresia, conjunctival bleeding with eyelid edema, teleangiectasia, Morbus Gaucher, sicklefoot, omphalocele, clubfoot, and stillbirth respectively.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Progesterone and 5 alpha-pregnane-3,20-dione in human amniotic fluid. 359 31

The ultrastructural response of the uterine luminal epithelium of the spayed virgin rat was studied as a parameter in screening the effects of antifertility agents which may interfere with implantation. The agents studied were bis-(p-acetoxyphenyl-2-methyl-cyclohexlidene-methane (F-6103), bis-(p-acetoxyphenyl)-2-methyl-4-methylidene-cyclohexylidene-methane (F- 6255), bis-(p-acetoxyphenyl)-1,2,3,4-tetrahydro-1-naphtylidene-methane ( F-6278), trans-(p-2-dimethylaminoethoxyphenyl) -1,2-diphenyl-1-ene (ICI- 46474), 1-(p-(2-diethylaminoethoxy) phenyl) -2-(p-methoxyphenyl-1-phenylethane (MER-25), 3-ethyl-2-methyl-4-pheny; -4-cyclohexenecarboxylic acid, sodium salt (ORF-4563), 1-(2-(p-(3,4,-dihydro-6-methoxy-2-phenyl-1-naphtyl)-phenoxy) ethyl)pyrro lidine, HCI(U-11100A), 2(p-(6-methoxy-2-phenylinden-3-yl) phenoxy)trieth ylamine, HCI (U-11555A) and 2-phenyl-1-p-(beta-pyrrolidinoethoxy) phenyl naphto(2,1-b)-furan (66/179). The substances were tested in spayed rats in spayed rats given progesterone and in spayed rats given progesterone plus estradiol-17 beta. All agents gave an estrogen-like response when given separatly. The response was most marked with the F-compounds and ORF-4563. The F-compounds and ORF-4563 changed the ultrastructure profoundly in progesterone-treated rats while the other compounds had little effect. Progesterone plus estradiol rendered the epithelium suitable for implantation. Each compound except U-1155A inhibited the attachment reaction when given before estradiol.
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PMID:Attachment reaction of rat uterine luminal epithelium. V. Suppression of the attachment reaction by some antifertility agents. 465 Jun 61

Medroxyprogesterone acetate (MPA; 5 micrograms/g body wt) or norethisterone oenanthate (NET-OEN; 4 micrograms/g body wt) was given to lactating female rats by subcutaneous injection 1 day after parturition. Each female suckled ten female pups which had been randomly allocated to her and at 21 days of age the pups were weaned. In this way female pups were exposed to either MPA or NET-OEN via milk during suckling. The patterns of LH and progesterone secretion at pro-oestrus were investigated using radioimmunoassay. When these pups reached adulthood it was found that neonatal exposure to MPA via milk significantly reduced the pro-oestrous LH peak by 45% as well as the total amount (by 27%) of LH secreted during pro-oestrus. Neonatal exposure via milk to NET-OEN had no effect on LH secretion during pro-oestrus. Pro-oestrous progesterone secretion was unaffected by either MPA or NET-OEN treatment.
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PMID:Neonatal exposure to a progestin via milk alters subsequent LH cyclicity in the female rat. 622 92

The time course of the concentration of the 14C- and 3H-labelled substances and of unchanged norethisterone was determined in maternal plasma and selected tissues of the feto-placental unit after intragastric administration of a combination of 14C-norethisterone acetate (NET-Ac) and 3H-ethinylestradiol (EE2), respective commercial formulation: Ostro - Primolut , to pregnant rats. When given intragastrically in doses of 1 mg NET-Ac/kg and 0.002 mg EE2/kg both synthetic steroids were rapidly and completely absorbed. Highest concentrations of 14C-labelled substances were measured 0.5 h p. admin . in maternal and fetal tissues. Only approximately 1% of total radioactivity in maternal plasma (= 30 ng NET/ml) corresponded to unchanged norethisterone. Less than 1% of the dose administered passed the placental barrier. The maximum NET-levels in the fetuses amounted to 4 ng NET/g tissue. The highest levels of EE2-metabolites in the fetuses were found 2-5 h after administration with 34 pg EE2-equiv./g corresponding to only 0.15% of the dose administered in total fetuses. 14C- and 3H-radioactivity was eliminated from the fetuses with a similar or only a slightly lower rate than from the maternal organism. When administered intragastrically the twofold dose (2 mg NET-Ac/kg plus 0.004 mg EE2/kg) to pregnant rhesus monkeys maximum NET plasma levels of 40 ng/ml were observed after 2 h. Thereafter the NET plasma levels decreased with a half-life of 1.4 hours. The time course of NET concentrations in ovary and pituitary mirrored plasma levels whereas that in placenta and amniotic fluid paralleled plasma levels at a 30-50% and 3-15% niveau , respectively.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Distribution of norethisterone and ethinylestradiol in the gravid rat and in the feto-placental unit of rhesus monkeys following intragastric administration of norethisterone acetate in combination with ethinylestradiol. I. Direct determinations. 654 Jan 2

The tissue distribution of 14C- and 3H-radioactivity was studied in pregnant rats and in fetuses of rhesus monkeys after intragastric administration of a combination of 14C-norethisterone acetate (14C-NET-Ac; 1 mg/kg rat, 2 mg/kg rhesus monkey) and of 3H-ethinyl-estradiol (3H-EE2; 2 micrograms/kg rat, 10 micrograms/kg rhesus monkey), respective commercial formulation: Ostro-Primolut, by means of autoradiographic methodology. The results of these present investigations confirm quantitative studies of a low, transitory passage of 14C-NET-Ac and 3H-EE2 into the fetuses. Within the fetuses the highest concentrations of 14C-radioactivity were found in the liver, in the vertebra, in heart and brain. No 3H-radioactivity could be observed within the fetuses. The autoradiographic studies do not indicate any specific enrichment of NET-Ac or EE2 and their metabolites in fetal organs and tissues.
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PMID:Distribution of norethisterone and ethinylestradiol in the gravid rat and in the feto-placental unit of rhesus monkeys following intragastric administration of norethisterone acetate in combination with ethinylestradiol. II. Autoradiography. 654 May 77

Depot-medroxyprogesterone acetate (DMPA) in a dose of 1-2 g per injection has been administered up to 3 times a week i.m. since the early 1960s for the prevention of miscarriage, but this therapy has proven unsuccessful. However, its use for contraception proved effective. Depot-norethindrone enanthate (NET-EN) was combined with DMPA in the late 1960s. NET-EN was injected every two months. In Germany, DMPA preparations made by the Upjohn Co. (Depot-Clinovir) and NET-EN made by the Schering Co. (Noristerat) are available for contraceptive purposes. Injectable gestagens are used in more than 80 countries worldwide, except for the US, because in studies on beagle dogs breast tumors developed. Injectables occupy a high share of contraceptives in developing countries: 8% in Kenya, 12% in Thailand, and almost 20% in Jamaica, while in central Europe the three-month injectable represents only 1% of contraceptive agents. In terms of pharmacokinetics, the maximum concentration of NET-EN is reached after an injection of 1 mg/kg i.m., averaging 2-5 ng/ml, which is over the 1 ng/ml dose required for contraceptive effectiveness. The bioavailability is 100% when so applied, while the elimination half-time is 15-20 days. A 1977 WHO study revealed a continuation rate of 70-75% after 12 months. About 10% complained of bleeding disorders. Within the first 6 months of DMPA use amenorrhea sets in in one-third of the cases; it occurs in over 60% of cases after 1-1.5 years of use. Bleeding disorders often cause discontinuation, which can be treated with estrogen-gestagen combination preparations. Dihydroxyprogesterone acetophenid is combined with estradiol enanthate (E2-EN), MPA with estradiol cypionate (E2-Cyp), NET-EN with estradiol valerate (E2-Val), and 17-alpha-hydroxyprogesterone caproate with E2-Val. The rate of continuation with the DMPA/estrogen combination was more than 60%, while it varied between 26.5% and 44.1% with NET-EN plus E2-Val after 1 year of use.
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PMID:[Depot gestagens]. 857 39


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