Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: DrugBank:APRD00627 (MAP)
 15,705 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Estradiol and testosterone both lowered endogenous liver glycogen and at 20-fold higher doses impaired triamcinolone acetonide mediated glyconeogenesis in adult adrenalectomized male rats. Neither steroid influenced liver tyrosine transaminase although tryptophan pyrrolase activity was depressed by testosterone. Progesterone increased liver tryptophan pyrrolase but did not influence other parameters. Cortexolone did not alter either of these processes whereas cortisol induced both enzymes and, at much higher dose levels, gluconeogenesis. Binding of 3H-triamcinolone acetonide to its cytoplasmic receptor in vitro was left unaffected in presence of 20-fold greater concentration of either sex steroid but almost totally abolished by cold, homologous molecules. Similar results were obtained by 3H-cortisol except that estradiol partially competed for 3H-cortisol binding sites even at 20-fold greater concentrations of cold estradiol. Separation on DEAE-cellulose-52 and Ultrogel 44 columns revealed binding of all steroids to macromolecules of comparable physicochemical properties although the ratios of binding to the various subpopulations of the receptor were a function of the steroid in question. These results are discussed in terms of sex steroid binding to different moieties of a complex, heterogeneous, polymorphic protein rather than inhibition of binding to the active configuration acquired in presence of an inducer.
Res Exp Med (Berl) 1979 Dec
PMID:Search for antiglucocorticoid activity in rat liver in vivo. 4 49

MAP was used in high doses (1 g/die up to a total dose of 45-50 g) in 44 cases of advanced mammary carcinoma (IIIrd and IVth stage of the T.N.M. classification), evaluated according to the criteria proposed by CBCG. The excellent tolerance to the drug, even at such high doses, is stressed. Therapeutic responses were best in cases of metastasis in the soft and bony tissues and in cases of pulmonary metastasis. It is pointed out that the effectiveness of the treatment is particularly evident in patients in whom the free interval has exceeded two years and in patients in the menopause for more than five years. In the light of results obtained, the possibility of introducing the drug into the therapeutic strategy of this condition is discussed.
Minerva Med 1977 Dec 01
PMID:[Use of high doses of medroxyprogesterone acetate in the palliative treatment of advanced breast cancer. Clinical experience with 44 cases]. 7 11

The McCormick Family Planning Program is a private, single-purpose program that has been offering contraceptive services to women in largely rural Chiang Mai province in Northern Thailand since 1963. In addition to two clinics in Chiang Mai city, the program operates a mobile unit, which visits service points throughout the province. An injectable contraceptive, DMPA, has been selected by about two-thirds of program acceptors since 1965, despite its prevalent side effect of amenorrhea. The service generates sufficient revenues, from relatively low fees for sterilization and contraception, to cover most operating costs. The program is seen as successful in providing rural women with contraceptives services. Aspects of the program--particularly the use of DMPA and the mobile service unit--are considered replicable in other settings.
Stud Fam Plann 1978 Dec
PMID:The McCormick Family Planning Program in Chiang Mai, Thailand. 10 32

The presence of a protein that binds specifically and with high affinity to progesterone is found in the plasma of fetal guinea Pig. Progesterone and 5 alpha-dihydroxyprogesterone strongly compete for the 3H-progesterone-protein complex. 5 beta-dihydroxy progesterone, 20 beta-dihydroxyprogesterone, testosterone and synthetic progestagen, R-5020 (17,21-dimethyl-19-norpregna-4, 9-diene-3,20 dione), also compete but less intensely. 17-hydroxyprogesterone, aldosterone, cortisol, oestradiol and oestrone have no effect. The 3H-progesterone-protein, complex has an affinity of Kd = 8.8 +/- 3.5 x 10(-10) M and in sucrose density gradient the sedimentation coefficient is 4.6 S.
C R Acad Hebd Seances Acad Sci D 1978 Dec
PMID:[Specific binding of 3H-progesterone to a plasma protein in the guinea pig fetus]. 11 16

The study was aimed at determining the possible role of long acting progesterone-DMPA in effecting reversal of the effect of TP on neonatally treated female Long-Evans rats. Five day-old female litters injected with 1.25 mg. TP went into persistent estrous on attaining maturity. DMPA when given in proper dosage and time reverted the condition.
Bangladesh Med Res Counc Bull 1979 Dec
PMID:Study of the effects of a long acting injectable-progesterone on the ovarian and uterine histomorphology of the androgenised female rats of Long-Evans strain. 16 73

Norethindrone (ENT), which is a representative in estrane series of progestogen, is not only strongly progestational but also estrogenic and in some cases, antiestrogenic. To understand progestational effect and antiestrogenic effect, the interactions of ENT on estrogen and progestogen receptors were studied in the uterine cytosol of white female rabbit. The 274,200 X G supernatant of uterine homogenate was used as cytosol. 3H-Estradiol, 3H-Progesterone, 3H-ENT or cold ENT were incubated with uterine cytosol at 4 degrees C for 2 hours. Results are as follows: 1. Sucrose gradient centrifugation [5 approximately 20% linear and 40,000 rpm (159,200 X G) for 16 hours at 4 degrees C]: ENT was bound to extrogen 8S receptor in immature rabbit uterus (Fig. 2 & 3), and to progestogen 8S receptor in estrogen primed rabbit uterus (Fig. 5). 2. Kinetic study, determined by dextran coated charcoal (0.001% dextran and 0.1% charcoal): (1) In the uterine cytosol of immature rabbit, 3H-estradiol-receptor binding was observed with Kd divide by 3.6 X 10-9 M and it was revealed that ENT was a competitive inhibitor to this binding with Ki divide by 2.6 X 10-6 M, as in Fig. 6. (2) 8S component, obtained by centrifugation of uterine cytosol (Fig. 1) in estrogen primed rabbit, binds 3H-progesterone with Kd divide by 8.1 X 10-10 M and Bm (maximal binding sites) divide by 5.0 X 10-8 M/mg of protein, and ENT was a competitive inhibitor in this binding with Ki divide by 2.3 X 10-9 M (FIG. 7 & 8). 3H-ENT-8S binding was demonstrated with Kd divide by 1.1 X 10-9 M and Bm divide by 8.7 X 10-8 M/mg of cytosol protein (Fig. 8). These results indicate: (a) ENT is bound to both estrogen and progestogen receptors in 8S macromolecules of uterine cytosol, (b) competitive inhibition of ENT to these bindings indicated that ENT is bound to these receptors at the steroid binding sites where estradiol and progesterone bind to, (c) ENT has much more affinity to progestogen receptor (Ki divide by 2.3 X 10-9 M) than to estrogen receptor (Ki divide 2.6 X 10-6 M), (d) while ENT is bound to progestogen and estrogen receptors at the same time, Bm of ENT (8.7 X 10-8 M/mg of cytosol protein) is more than Bm of progesterone (5.0 X 10-9 M/mg of cytosol protein), and Kd of ENT (1.1 X 10-9 M) was less than Ki of ENT (2.3 X 10-9 M) in the binding to progesterone-receptor. Biologically, while ENT is bound to progestogen -receptor with high affinity and to estrogen receptor with low affinity, ENT is actually progestational in low dose and antiestrogenic in high dose but the anti-estrogenicity seems to be incomplete in vivo as ENT may be metabolized to a potent estrogenic compound, ethinyl estradiol
Nihon Naibunpi Gakkai Zasshi 1975 Dec 20
PMID:[Interaction of norethindrone on estrogen and progesterone receptors in the rabbit uterine cytosol (author's transl)]. 18 90

Estrogen priming increases uterine 8S macromolecule which binds progesterone specifically. Progesterone-8S complex in the cytoplasm enters into nucleus and is bound to chromatin finally. In this paper, the mode of nuclear translocation of steroid in exchange assay of receptor introduced by Anderson et al., and the mode of binding to chromatin were studied on the progesterone-receptor complex in the uterus of estrogen primed female rabbit. 1. After intravenous administration of 200 mug progesterone into the estrogen primed immature rabbit, uterine nuclei were prepared by the method in Table 1. These nuclei were incubated with 3H-progesterone and cold steroids at 4 degrees C for 30 minutes, and then washed with buffer A. The radioactivity of the nuclei was counted. This experiment was performed at 4 degrees C because progesterone receptor and chromatin were observed to be degraded at 37 degrees C for 20 minutes. The effect of cold steroids in vitro on the incorporation of 3H-progesterone into the uterine nuclei of rabbit pretreated with progesterone was found to be similar to their effect on progesterone-receptor binding in cytosol or chromatin (Fig. 1). 2. The effect of cold steroids on 3H-progesterone-receptor-chromatin triplex (Table 2 and Fig. 2) was examined. Once 3H-progesterone-receptor-chromatin triplex was formed, it was difficult to exchange 3H-progesterone to other steroids at 4 degrees C. These results (1 & 2) indicate that progesterone-receptor complex enters into nucleus and is bound to chromatin. Exchange of steroid may occur in the nuclear progesterone-receptor complex, which is free from the binding with chromatin. And thus exchange assay cannot represent quantitative data on receptor content. 3. 3H-progesterone-8S or 5S complexes were obtained by 5 approximately 20% sucrose linear gradient centrifugation (Fig. 3). The same molar concentration of these complexes from estrogen primed or castrated rabbit uterus were incubated with primed uterine chromatin for 30 minutes. Then the chromatin was washed with buffer A and the radioactivity was counted. It was shown in Fig. 4 that 3H-progesterone-8S complex was bound to chromatin much more tightly than 3H-progesterone 5-S complex in preparations obtained from both castrated or primed uterine cytosols. All these results indicate that 8S may be the biologically active form of the receptor. 4.3H-progesterone uptake into uterine nuclei was observed in very limited amount following the injection into uterine artery. The radioactivity in nuclei decreased easily by washing with buffer A as in Fig. 5. The small amount of residual radioactivity after washing, that is, very limited number of binding sites with high affinity is considered to be indicative of biologically active binding.
Nihon Naibunpi Gakkai Zasshi 1975 Dec 20
PMID:[Studies on progesterone receptor in rabbit uterine cytosol -- nuclear translocation and chromatin binding-- (author's transl)]. 18 91

The possibility that mean arterial pressure (MA) might be maintained by an effect of angiotensin II or its precursors on the central nervous system in rats made hypertensive by occluding the aorta between the renal arteries was investigated. Aortic coarctation produced severe hypertension (MAP greater than 150 mmHg) and plasma renin activity values (radioimmunoassay) at least 10 times normal within 2-6 days after surgery. [Sar1, IIe8]angiotensin II, an angiotensin II antagonist administered centrally via an intracerebroventricular (icv) injection (10-100 mug), lowered the MAP in a dose-dependent manner. Peripheral administration of [Sar1, IIe8]angiotensin II (bolus injection) at 100 mug intra-arterially was ineffective, but the antagonist did lower arterial pressure when infused intravenously for 1 h at 4 times this dose. Less than Glu-Trp-Pro-Arg-Pro-Gln-Ile-Pro-Pro, a converting enzyme inhibitor, and pepstatin, a renin inhibitor, were ineffective via an icv injection. These results suggest that angiotensin II is in part responsible for the elevation in blood pressure following aortic coarctation in rats. Both central and peripheral administration of [Sar1, Ile8]-angiotensin II lowered mean arterial pressure but the antagonist lowered arterial pressure at lower doses and produced a more rapid decline in arterial pressure when administered into the central nervous system then when administered intra-arterially or intravenously.
Am J Physiol 1976 Dec
PMID:Central antihypertensive effects of inhibitors of the renin-angiotensin system in rats. 18 43

The maturation of the amphibian oocyte has been analyzed. Progesterone as well as organomercurials, lanthanum chloride and propranolol rapidly induce maturation. These chemicals are active only is applied on the cell surface. The mechanism seems to be an induction of the migration of Ca2+ from the cell membrane to the cytoplasm. K + may also play a role. Progesterone induced maturation involves synthesis of histone and histone kinase as well as several biologically active but chemically unidentified factors. cAMP does not seem to be directly involved, whereas protein phosphorylation is so.
Med Biol 1978 Dec
PMID:The hormonal induction of maturation in amphibian oocytes. 21 52

Mechanical firmness of 4 UV hardened composites was estimated by the bending test according to DIN 13922. Bending strength and breaking point lie between 70 and 120 MPA and 0.5 and 0.25 mm compared with 110 MPA and 0.13 mm for Adaptic. The results show that the combination of filling substance and UV irradiation is well balanced.
Dtsch Zahnarztl Z 1977 Dec
PMID:[Bending strength of UV hardening composites]. 27 75


1 2 3 4 5 6 7 8 9 10 Next >>