Cyclofenil
Chondrosarcoma
A slowly growing malignant neoplasm derived from cartilage cells, occurring most frequently in pelvic bones or near the ends of long bones, in middle-aged and old people. Most chondrosarcomas arise de novo, but some may develop in a preexisting benign cartilaginous lesion or in patients with ENCHONDROMATOSIS. (Stedman, 25th ed)
Chondroitin Sulfates
Derivatives of chondroitin which have a sulfate moiety esterified to the galactosamine moiety of chondroitin. Chondroitin sulfate A, or chondroitin 4-sulfate, and chondroitin sulfate C, or chondroitin 6-sulfate, have the sulfate esterified in the 4- and 6-positions, respectively. Chondroitin sulfate B (beta heparin; DERMATAN SULFATE) is a misnomer and this compound is not a true chondroitin sulfate.
Estrogens
Compounds that interact with ESTROGEN RECEPTORS in target tissues to bring about the effects similar to those of ESTRADIOL. Estrogens stimulate the female reproductive organs, and the development of secondary female SEX CHARACTERISTICS. Estrogenic chemicals include natural, synthetic, steroidal, or non-steroidal compounds.
Receptors, Estrogen
Estrogen Receptor alpha
Estrogen Receptor beta
Estradiol
Neoplasms
Structural Homology, Protein
Models, Molecular
Templates, Genetic
Computer Graphics
User-Computer Interface
Leukemia, Myelogenous, Chronic, BCR-ABL Positive
Clonal hematopoetic disorder caused by an acquired genetic defect in PLURIPOTENT STEM CELLS. It starts in MYELOID CELLS of the bone marrow, invades the blood and then other organs. The condition progresses from a stable, more indolent, chronic phase (LEUKEMIA, MYELOID, CHRONIC PHASE) lasting up to 7 years, to an advanced phase composed of an accelerated phase (LEUKEMIA, MYELOID, ACCELERATED PHASE) and BLAST CRISIS.
K562 Cells
Fusion Proteins, bcr-abl
Translation products of a fusion gene derived from CHROMOSOMAL TRANSLOCATION of C-ABL GENES to the genetic locus of the breakpoint cluster region gene on chromosome 22. Several different variants of the bcr-abl fusion proteins occur depending upon the precise location of the chromosomal breakpoint. These variants can be associated with distinct subtypes of leukemias such as PRECURSOR CELL LYMPHOBLASTIC LEUKEMIA-LYMPHOMA; LEUKEMIA, MYELOGENOUS, CHRONIC, BCR-ABL POSITIVE; and NEUTROPHILIC LEUKEMIA, CHRONIC.
Transcriptome
Sezary Syndrome
Aortic Valve Prolapse
Sports Medicine
Doping in Sports
Anovulation
Ovulation Induction
Pituitary Gland
Gonadotropins
Hormones that stimulate gonadal functions such as GAMETOGENESIS and sex steroid hormone production in the OVARY and the TESTIS. Major gonadotropins are glycoproteins produced primarily by the adenohypophysis (GONADOTROPINS, PITUITARY) and the placenta (CHORIONIC GONADOTROPIN). In some species, pituitary PROLACTIN and PLACENTAL LACTOGEN exert some luteotropic activities.
Gonadotropins, Pituitary
Hormones secreted by the adenohypophysis (PITUITARY GLAND, ANTERIOR) that stimulate gonadal functions in both males and females. They include FOLLICLE STIMULATING HORMONE that stimulates germ cell maturation (OOGENESIS; SPERMATOGENESIS), and LUTEINIZING HORMONE that stimulates the production of sex steroids (ESTROGENS; PROGESTERONE; ANDROGENS).
Fluorine-substituted cyclofenil derivatives as estrogen receptor ligands: synthesis and structure-affinity relationship study of potential positron emission tomography agents for imaging estrogen receptors in breast cancer. (1/10)
In a search for estrogen receptor (ER) ligands to be radiolabeled with fluorine-18 for imaging of ER-positive breast tumors with positron emission tomography (PET), we investigated cyclofenil analogues substituted at the C3 or C4 position of the cyclohexyl group. McMurry coupling of 4,4'-dihydroxybenzophenone with various ketones produced key cyclofenil intermediates, from which C3 and C4 substituents containing alkyl and various oxygen or fluorine-substituted alkyl groups were elaborated. Binding assays to both ERalpha and ERbeta revealed that the C3 site is more tolerant of steric bulk and polar groups than the C4 site, consistent with a computational model of the ERalpha ligand binding pocket. Fluorine substitution is tolerated very well at some sites, giving some compounds having affinities comparable to or higher than that of estradiol. These fluoro and fluoroalkyl cyclofenils merit further consideration as fluorine-18 labeled ER ligands for PET imaging of ERs in breast tumors. (+info)Effects of cyclofenil diphenol, an agent which disrupts Golgi structure, on proteoglycan synthesis in chondrocytes. (2/10)
1. Cyclofenil diphenol (F6060), a weak non-steroidal oestrogen, was shown previously to inhibit [35S]proteoglycan synthesis [Mason, Lineham, Phillipson & Black (1984) Biochem. J. 223, 401-412] and to induce fragmentation of the Golgi apparatus into small vesicles [Lancaster, Fryer, Griffiths & Mason (1989) J. Cell Sci. 92, 271-280] in cultures of Swarm chondrosarcoma chondrocytes. Two structurally related compounds, F6204 and F6091, show a similar concentration-related effect, with complete inhibition of [35S]proteoglycan synthesis at 90 micrograms/ml. The apparent [3H]protein synthesis is only approx. 40% inhibited with [3H]lysine as precursor. Stilboestrol, clomiphene and tamoxiphen are also potent inhibitors of [35S]proteoglycan synthesis. 2. Syntheses of chondroitin 4-[35S]sulphate and chondroitin 6-[35S]sulphate, which are Golgi-mediated events, are inhibited 40-68% and 3-48% respectively by concentrations of cyclofenil between 50 and 70 micrograms/ml. [3H]Hyaluronan synthesis, which occurs by a different mechanism at the plasma membrane, is inhibited by 47-66%. These results suggest that cyclofenil may act via more than one inhibitory mechanism. Cyclofenil diphenol inhibits polymerization of chondroitin sulphate on to p-nitrophenyl beta-xyloside even when the chondrocytes are loaded with the initiator prior to treatment. 3. Cyclofenil diphenol interferes with the cellular uptake of amino acids via the system A carrier, as shown by inhibition of uptake of methylaminoisobutyric acid, a specific substrate for this system. The drug had no effect on the uptake of 2-deoxyglucose by the cells. 4. Cyclofenil diphenol (90 micrograms/ml) caused a decrease in the pool size of UDP-N-acetylglucosamine, UDP-N-acetylgalactosamine and UDP-hexoses, but this was insufficient to account for the accompanying profound inhibition of [35S]proteoglycan synthesis. Entry of [3H]glucosamine into the cell and into the UDP-N-acetylhexosamine pool did not appear to be affected. 5. Cyclofenil diphenol inhibited the substitution of 3H-labelled proteoglycan core protein with chondroitin sulphate chains. Core protein was identified in treated cultures on the basis of immunoprecipitation with an antiserum against the hyaluronate-binding region and distinguished from precipitated proteoglycan on SDS/PAGE. (+info)Synthesis and biodistribution of fluorine-18-labeled fluorocyclofenils for imaging the estrogen receptor. (3/10)
C4-[18F]Fluorocyclofenil ([18F]FCF, 6) and C3-[18F]fluoroethylcyclofenil ([18F]FECF, 9), two high-affinity nonsteroidal estrogens, were prepared and investigated as potential agents for imaging estrogen receptors (ERs) in breast tumors. Both of these compounds could be prepared conveniently from alkyl methanesulfonate precursors (5,8) by fluoride displacement reactions, and they were obtained in high radiochemical purity and radiochemical yields, with effective specific activities sufficient for in vivo biodistribution studies. While the biodistribution of [18F]FCF (6) in immature female rats showed no selective target tissue uptake, the biodistribution of [18F]FECF (9) showed selective uptake by the uterus, but this uptake could not be blocked by excess estradiol. The poor in vivo biodistribution of these otherwise high-affinity ligands arouses curiosity, and together with recent results on the biodistribution of other nonsteroidal ligands suggests that factors other than receptor binding affinity are important for in vivo imaging of estrogen target tissues and ER-positive breast tumors. (+info)Nonclassical SNAPFL analogue as a Cy5 resonance energy transfer partner. (4/10)
(+info)Monitoring a coordinated exchange process in a four-component biological interaction system: development of a time-resolved terbium-based one-donor/three-acceptor multicolor FRET system. (5/10)
(+info)Characterization of the pharmacophore properties of novel selective estrogen receptor downregulators (SERDs). (6/10)
(+info)Ultrastructural changes accompany inhibition of proteoglycan synthesis in chondrocytes by Cyclofenil diphenol. (7/10)
Cyclofenil diphenol, a weak non-steroidal oestrogen, profoundly inhibits [35S]proteoglycan synthesis in cultures of Swarm chondrosarcoma chondrocytes under conditions in which protein synthesis is only marginally reduced. In the present experiments it was shown that after a 40-min treatment with Cyclofenil diphenol (90 micrograms ml-1) most of the normally abundant Golgi stacks in these cells disappeared and after 60 min they were absent. After 2-3 h treatment the cisternae of the endoplasmic reticulum (ER) were grossly distended and transformed into large ribosome-studded vesicles containing flocculent and filamentous material. These changes were dependent on the concentration of Cyclofenil and were fully reversible within 21 h of withdrawing the drug. The ultrastructural changes differed in some aspects if protein synthesis was blocked with cycloheximide for 15 min or 180 min before and during treatment with Cyclofenil. The Golgi disappeared but the ER cisternae, though distended, formed a continuous network and swollen ribosome-studded vesicles did not develop. However, non-membrane-bounded structures containing lipid droplets and material of low electron density developed in the cytoplasm under these conditions. The ultrastructural changes induced by Cyclofenil differ from those induced by monensin and diethylcarbamazine, suggesting that the drug acts at a different point in the secretory pathway for macromolecules. (+info)Selective inhibition of proteoglycan and hyaluronate synthesis in chondrocyte cultures by cyclofenil diphenol, a non-steroidal weak oestrogen. (8/10)
Cyclofenil diphenol, a weak non-steroidal oestrogen, binds to albumin. In the presence of concentrations of albumin just sufficient to keep cyclofenil diphenol in solution, the compound inhibited the synthesis of [35S]proteoglycans, [3H]glycoproteins, [3H]hyaluronate and [3H]proteins in primary cultures of chondrocytes from the Swarm rat chondrosarcoma in a dose-dependent manner. When excess albumin was present, conditions were found (90 micrograms of cyclofenil diphenol and 4 mg of albumin per ml of culture medium) which completely inhibited [35S]proteoglycan and [3H]hyaluronate synthesis but had little effect on [3H]protein or [3H]glycoprotein synthesis. The time of onset of inhibition of [35S]proteoglycan synthesis by cyclofenil diphenol was very rapid (t1/2 less than 25 min) and incompatible with an action mediated through suppression of proteoglycan core protein synthesis. Cyclofenil diphenol inhibited the synthesis of [35S]chondroitin sulphate chains onto p-nitrophenyl beta-D-xyloside in the cultures. Cyclofenil diphenol had little effect on the secretion from chondrocytes of [35S]proteoglycans synthesized immediately prior to treatment. Chondrocyte cultures treated with cyclofenil diphenol recovered their biosynthetic activities almost completely within 3 h of removing the compound from the culture medium. Cyclofenil diphenol had a similar inhibitory action on the synthesis of [35S]proteoglycans in secondary cultures of human dermal fibroblasts from both normal subjects and patients with systemic sclerosis. It is proposed that cyclofenil diphenol inhibits the synthesis of [35S]proteoglycans by interfering with the formation of the glycosaminoglycan side chains of these molecules in the Golgi apparatus of cells. The action may be due to disturbance of Golgi membrane organization by the compound. (+info)
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List of drugs banned by WADA
Clomiphene, cyclofenil, fulvestrant, and all other anti-estrogenic substances are banned. Myostatin inhibitors are banned. ...
4,4'-Dihydroxybenzophenone
McMurry reaction between CHone and p,p′-dihydroxybenzophenone, and subsequent acetylation gives Cyclofenil. Eddine, Ali Nasser ...
Endoxifen
"Novel Selective Estrogen Receptor Ligand Conjugates Incorporating Endoxifen-Combretastatin and Cyclofenil-Combretastatin Hybrid ...
Bisacodyl
Diphenyl-2-pyridylmethane Cyclofenil Wexner SD, Beck DE, Baron TH, Fanelli RD, Hyman N, Shen B, Wasco KE (June 2006). "A ...
List of banned substances in baseball
... cyclofenil, and fulvestrant Adrafinil Amfepramone (diethylproprion) Amiphenazole Amphetamine Amphetaminil Armodafinil ...
Sex-hormonal agent
... cyclofenil, raloxifene, toremifene, lasofoxifene, ospemifene, bazedoxifene Antiestrogens (ER antagonists) Examples: fulvestrant ...
Nonsteroidal
... cyclofenil, droloxifene, enclomifene, endoxifen, ethamoxytriphetol, fispemifene, idoxifene, lasofoxifene, levormeloxifene, ...
List of selective estrogen receptor modulators
... cyclofenil (Sexovid), lasofoxifene (Fablyn), ormeloxifene (Centron, Novex, Novex-DS, Sevista), ospemifene (Osphena; ...
List of drugs: Cp-Cz
Cyclocort cyclofenil (INN) cycloguanil embonate (INN) Cyclogyl Cyclomen. Redirects to Danazol. cyclomenol (INN) cyclomethycaine ...
ATC code G03
... combinations G03GB01 Cyclofenil G03GB02 Clomifene G03GB03 Epimestrol G03HA01 Cyproterone G03HB01 Cyproterone and estrogen ...
Cyclofenil
... is the English generic name of the drug and its INN, USAN, and BAN. Cyclofenil has been marketed under a variety of ... Cyclofenil has been available in the form of 100, 200, and 400 mg oral tablets. Cyclofenil has been used by male athletes to ... The elimination half-life of cyclofenil after a single 200 mg dose is 18 to 29 hours. Cyclofenil is a nonsteroidal SERM and is ... In men, cyclofenil can increase testosterone levels due its progonadotropic effects. In terms of distribution, cyclofenil acts ...
4-Hydroxyestrone
Notes: Values are mean ± SD or range. ER RBA = Relative binding affinity to estrogen receptors of rat uterine cytosol. Uterine weight = Percentage change in uterine wet weight of ovariectomized rats after 72 hours with continuous administration of 1 μg/hour via subcutaneously implanted osmotic pumps. LH levels = Luteinizing hormone levels relative to baseline of ovariectomized rats after 24 to 72 hours of continuous administration via subcutaneous implant. Footnotes: a = Synthetic (i.e., not endogenous). b = Atypical uterotrophic effect which plateaus within 48 hours (estradiol's uterotrophy continues linearly up to 72 hours). Sources: See template ...
Acolbifene
InChI=1S/C29H31NO4/c1-20-26-14-11-24(32)19-27(26)34-29(28(20)21-5-9-23(31)10-6-21)22-7-12-25(13-8-22)33-18-17-30-15-3-2-4-16-30/h5-14,19,29,31-32H,2-4,15-18H2,1H3/t29-/m0/ ...
Prolame
Rubio-Póo C, Mandoki JJ, Mendoza-Patiño N, Lemini C, de la Peña A, Cruz F, Zavala E, Silva G, Garcia-Mondragón J, Fernández JM (1985). "The anticoagulant effect of prolame, N-(3-hydroxy-1,3,5(10)estratrien-17 beta-yl)-3-hydroxypropylamine, a novel amino-estrogen". Steroids. 45 (2): 159-70. PMID 3841425 ...
Estrobin
... , also known as α,α-di(p-ethoxyphenyl)-β-phenylbromoethylene and commonly abbreviated as DBE, is a synthetic, nonsteroidal estrogen of the triphenylethylene group that was never marketed.[1][2] Chlorotrianisene, and subsequently clomifene and tamoxifen, were derived from it.[1][2] Estrobin, similarly to other triphenylethylenes, is very lipophilic and hence very long-lasting in its duration of action.[1][2] Similarly to chlorotrianisene, estrobin behaves a prodrug to a much more potent estrogen in the body.[2] ...
Hormone replacement therapy
The Women's Health Initiative trials were conducted between 1991 and 2006 and were the first large, double-blind, placebo-controlled clinical trials of HRT in healthy women.[52] Their results were both positive and negative, suggesting that during the time of hormone therapy itself, there are increases in invasive breast cancer, stroke and lung clots. Other risks include increased endometrial cancer, gallbladder disease, and urinary incontinence, while benefits include decreased hip fractures, decreased incidence of diabetes, and improvement of vasomotor symptoms. There also is an increased risk of dementia with HRT in women over 65, though when given earlier it appears to be neuroprotective. After the cessation of HRT, the WHI continued observe its participants, and found that most of these risks and benefits dissipated, though some elevation in breast cancer risk did persist.[24] Other studies have also suggested an increased risk of ovarian cancer.[43] The arm of the WHI receiving combined ...
Androstenediol
... has been investigated for use as a radiation countermeasure. Its value as a radiation countermeasure is based mainly on its stimulation of production of white blood cells and platelets.[6] Its potential use as a radiation countermeasure was developed by the Armed Forces Radiobiology Research Institute (AFRRI) and subsequently studied by AFRRI and Hollis-Eden Pharmaceuticals under the proposed brand name Neumune for the treatment of acute radiation syndrome.[6][7] The clinical trials with rhesus monkeys were successful. According to the Hollis-Eden report, only 12.5% of the 40 Neumune-treated animals died versus 32.5% in the placebo group.[8] Hollis-Eden had applied for a contract from the U.S. Government under the BioShield Request for Proposals (RFP) for radiation countermeasures. After being encouraged for 2.5 years that Neumune was in the competitive range, on March 9, 2007, the RFP was canceled by HHS. According to HHS, "the product was no longer in the competitive ...
Norethisterone
Due to its weak androgenic activity, norethisterone can produce androgenic side effects such as acne, hirsutism, and voice changes of slight severity in some women at high dosages (e.g., 10 to 40 mg/day).[8] This is notably not the case with combined oral contraceptives that contain norethisterone and EE, however.[9] Such formulations contain low dosages of norethisterone (0.35 to 1 mg/day)[9] in combination with estrogen and are actually associated with improvement in acne symptoms.[25][26] In accordance, they are in fact approved by the FDA for the treatment of acne in women in the United States.[25][26] The improvement in acne symptoms is believed to be due to a 2- to 3-fold increase in sex hormone-binding globulin (SHBG) levels and a consequent decrease in free testosterone levels caused by EE, which results in an overall decrease in androgenic signaling in the body.[27] The sebaceous glands are highly androgen-sensitive and their size and activity are potential markers of androgenic ...
GPER
The classical estrogen receptors first characterized in 1958[6] are water-soluble proteins located in the interior of cells that are activated by estrogenenic hormones such as estradiol and several of its metabolites such as estrone or estriol. These proteins belong to the nuclear hormone receptor class of transcription factors that regulate gene transcription. Since it takes time for genes to be transcribed into RNA and translated into protein, the effects of estrogens binding to these classical estrogen receptors is delayed. However, estrogens are also known to have effects that are too fast to be caused by regulation of gene transcription.[7] In 2005, it was discovered that a member of the G protein-coupled receptor (GPCR) family, GPR30 also binds with high affinity to estradiol and is responsible in part for the rapid non-genomic actions of estradiol. Based on its ability to bind estradiol, GPR30 was renamed as G protein-coupled estrogen receptor (GPER). Unlike the other members of the GPCR ...
Promestriene
... (INN) (brand names Colpotrofin, Colpotrophine, Delipoderm), also known as estradiol 3-propyl 17β-methyl diether, is a synthetic steroidal estrogen which is used topically in a 1% cream formulation.[1][2][3][4] It is the 3-propyl and 17β-methyl diether of estradiol.[5] The drug is described as a tropic agent and antiseborrheic.[1] It has not been found to be effective in the treatment of androgenic alopecia or other conditions of cutaneous androgenization.[6][7] ...
Rhaponticin
InChI=1S/C21H24O9/c1-28-16-5-4-11(8-15(16)24)2-3-12-6-13(23)9-14(7-12)29-21-20(27)19(26)18(25)17(10-22)30-21/h2-9,17-27H,10H2,1H3/b3-2+/t17-,18-,19+,20-,21-/m1/s1 ...
Estriol
... is produced in quantities that are notable only during pregnancy.[3] Levels of estriol increase 1,000-fold during pregnancy,[8] whereas levels of estradiol and estrone increase 100-fold,[12] and estriol accounts for 90% of the estrogens in the urine of pregnant women.[5] At term, the daily production of estriol by the placenta is 35 to 45 mg,[12] and levels in the maternal circulation are 8 to 13 ng/dL.[3] The placenta produces pregnenolone and progesterone from circulating cholesterol.[4] Pregnenolone is taken up by the fetal adrenal glands and converted into dehydroepiandrosterone (DHEA), which is then sulfated by steroid sulfotransferase into dehydroepiandrosterone sulfate (DHEA-S).[citation needed] DHEA-S is hydroxylated by high CYP3A7 expression and activity into 16α-hydroxy-DHEA-S (16α-OH-DHEA-S) in the fetal liver and to a limited extent in the fetal adrenal glands.[3][18] 16α-OH-DHEA-S is then taken up by the placenta.[3] Due to high expression of steroid sulfatase in the ...
Estradiol
Levels of estradiol in premenopausal women are highly variable throughout the menstrual cycle and reference ranges widely vary from source to source.[59] Estradiol levels are minimal and according to most laboratories range from 20 to 80 pg/mL during the early to mid follicular phase (or the first week of the menstrual cycle, also known as menses).[60][61] Levels of estradiol gradually increase during this time and through the mid to late follicular phase (or the second week of the menstrual cycle) until the pre-ovulatory phase.[59][60] At the time of pre-ovulation (a period of about 24 to 48 hours), estradiol levels briefly surge and reach their highest concentrations of any other time during the menstrual cycle.[59] Circulating levels are typically between 130 and 200 pg/mL at this time, but in some women may be as high as 300 to 400 pg/mL, and the upper limit of the reference range of some laboratories are even greater (for instance, 750 pg/mL).[59][60][62][63][64] Following ovulation (or ...
Methoxychlor
Human exposure to methoxychlor occurs via air, soil, and water,[7] primarily in people who work with the substance or who are exposed to air, soil, or water that has been contaminated. It is unknown how quickly and efficiently the substance is absorbed by humans who have been exposed to contaminated air or via skin contact.[7] In animal models, high doses can lead to neurotoxicity.[7] Some methoxychlor's metabolites have estrogenic effects in adult and developing animals before and after birth.[7] One studied metabolite is 2,2-bis(p-hydroxyphenyl)-1,1,1-trichloroethane (HPTE) which shows reproductive toxicity in an animal model by reducing testosterone biosynthesis.[8][9] Such effects adversely affect both the male and female reproductive systems. It is expected that this "could occur in humans" but has not been proven.[7] While one study has linked methoxychlor to the development of leukemia in humans, most studies in animals and humans have been negative, thus the EPA has determined that it is ...
Androstanolone
... is a potent agonist of the AR. It has an affinity (Kd) of 0.25 to 0.5 nM for the human AR, which is about 2- to 3-fold higher than that of testosterone (Kd = 0.4 to 1.0 nM)[39] and the dissociation rate of androstanolone from the AR is also about 5-fold slower than that of testosterone.[40] The EC50 of androstanolone for activation of the AR is 0.13 nM, which is about 5-fold stronger than that of testosterone (EC50 = 0.66 nM).[41] In bioassays, androstanolone has been found to be 2.5- to 10-fold more potent than testosterone.[39] Unlike testosterone and various other AAS, androstanolone cannot be aromatized, and for this reason, poses no risk of estrogenic side effects like gynecomastia at any dosage.[42] In addition, androstanolone cannot be metabolized by 5α-reductase (as it is already 5α-reduced), and for this reason, is not potentiated in so-called "androgenic" tissues like the skin, hair follicles, and prostate gland, thereby improving its ratio of anabolic to androgenic ...
Antiestrogen
... s include selective estrogen receptor modulators (SERMs) like tamoxifen, clomifene, and raloxifene, the ER silent antagonist and selective estrogen receptor degrader (SERD) fulvestrant,[4][5] aromatase inhibitors (AIs) like anastrozole, and antigonadotropins including androgens/anabolic steroids, progestogens, and GnRH analogues. Although aromatase inhibitors and antigonadotropins can be considered antiestrogens by some definitions, they are often treated as distinct classes.[6] Aromatase inhibitors and antigonadotropins reduce the production of estrogen, while the term "antiestrogen" is often reserved for agents reducing the response to estrogen.[7] ...
Danazol
... is known to bind to two steroid hormone carrier proteins: sex hormone-binding globulin (SHBG), which binds androgens and estrogens; and corticosteroid-binding globulin (CBG), which binds progesterone and cortisol.[5][6] Binding of danazol to SHBG is considered to be more important clinically.[6] By occupying SHBG and CBG, danazol increases the ratio of free to plasma protein-bound testosterone, estradiol, progesterone, and cortisol.[5][6] The table to the right shows the difference in testosterone levels in premenopausal women treated with danazol.[6] As can be seen, the percentage of free testosterone is tripled in women being treated with danazol.[6][34] The ability of danazol to increase free testosterone levels suggests that a portion of its weak androgenic effects are mediated indirectly by facilitating the activity of testosterone and dihydrotestosterone through the displacement of them from SHBG.[6][34] In addition to binding to and occupying SHBG however, danazol also decreases ...
Polyestradiol phosphate
PEP produces minimal undesirable effects on coagulation factors and is thought to increase the risk of blood clots little or not at all.[28][29] This is in spite of the fact that estradiol levels can reach high concentrations of as much as 700 pg/mL with high-dose (320 mg/month) PEP therapy.[30] It is also in contrast to oral synthetic estrogens such as diethylstilbestrol and ethinylestradiol, which produce marked increases in coagulation factors and high rates of blood clots at the high doses used to achieve castrate levels of testosterone in prostate cancer.[28][29][6] The difference between the two types of therapies is due to the bioidentical and parenteral nature of PEP and its minimal influence on liver protein synthesis.[28][29][6] PEP might actually reduce the risk of blood clots, due to decreases in levels of certain procoagulatory proteins.[28][29] Although PEP does not increase the hepatic production or levels of procoagulatory factors, it has been found to significantly decrease ...
Ethinylestradiol/levonorgestrel
... (also ethinyl estradiol/levonorgestrel) is a combined birth control pill made up of ethinylestradiol, an estrogen and levonorgestrel a progestin.[2] It is used for birth control, symptoms of menstruation, endometriosis, and as emergency contraception.[1][2] It is taken by mouth.[1] Side effects can include nausea, headache, blood clots, breast pain, depression, and liver problems.[2] Use is not recommended during pregnancy, the initial three weeks after childbirth, and in those at high risk of blood clots.[2] However, it may be started immediately after a miscarriage or abortion.[3] Smoking while using combined birth control pills is not recommended.[1] It works by stopping ovulation, making the mucus at the opening to the cervix thick, and making the uterus not suitable for implantation.[1] Ethinylestradiol/levonorgestrel has been approved for medical use in the United States at least since 1982.[1] It is on the World Health Organization's List of Essential ...
8,9-Dehydroestrone
... , or Δ8-estrone, also known as estra-1,3,5(10),8-tetraen-3-ol-17-one, is a naturally occurring estrogen found in horses which is closely related to equilin, equilenin, and estrone, and, as the 3-sulfate ester sodium salt, is a minor constituent (3.5%) of conjugated estrogens (Premarin).[1][2][3][4] It produces 8,9-dehydro-17β-estradiol as an important active metabolite, analogously to conversion of estrone or estrone sulfate into estradiol.[2][4][5][3] The compound was first described in 1997.[6][3] In addition to 8,9-dehydroestrone and 8,9-dehydro-17β-estradiol, 8,9-dehydro-17α-estradiol is likely also to be present in conjugated estrogens, but has not been identified at this time.[2] ...
RCSB PDB - 5DZ1: Crystal Structure of the ER-alpha Ligand-binding Domain in Complex with the Cyclofenil Derivative 4,4'-[(4...
RCSB PDB - 5E14: Crystal Structure of the ER-alpha Ligand-binding Domain in Complex with the Cyclofenil Derivative 4,4'-{[(3R)...
Cyclofenil - Wikipedia
Cyclofenil is the English generic name of the drug and its INN, USAN, and BAN. Cyclofenil has been marketed under a variety of ... Cyclofenil has been available in the form of 100, 200, and 400 mg oral tablets. Cyclofenil has been used by male athletes to ... The elimination half-life of cyclofenil after a single 200 mg dose is 18 to 29 hours. Cyclofenil is a nonsteroidal SERM and is ... In men, cyclofenil can increase testosterone levels due its progonadotropic effects. In terms of distribution, cyclofenil acts ...
Fluorine-substituted cyclofenil derivatives as estrogen receptor ligands: Synthesis and structure-affinity relationship study...
Fluorine-substituted cyclofenil derivatives as estrogen receptor ligands: Synthesis and structure-affinity relationship study ... T1 - Fluorine-substituted cyclofenil derivatives as estrogen receptor ligands. T2 - Synthesis and structure-affinity ... Fluorine-substituted cyclofenil derivatives as estrogen receptor ligands: Synthesis and structure-affinity relationship study ... Fluorine-substituted cyclofenil derivatives as estrogen receptor ligands : Synthesis and structure-affinity relationship study ...
An estrogen antagonist, cyclofenil, has anti-dengue-virus activity<...
Cyclofenil also inhibited the replication of Zika virus. A time-of-addition assay suggested that cyclofenil may interfere with ... Cyclofenil also inhibited the replication of Zika virus. A time-of-addition assay suggested that cyclofenil may interfere with ... Cyclofenil also inhibited the replication of Zika virus. A time-of-addition assay suggested that cyclofenil may interfere with ... Cyclofenil also inhibited the replication of Zika virus. A time-of-addition assay suggested that cyclofenil may interfere with ...
An estrogen antagonist, cyclofenil, has anti-dengue-virus activity - Fingerprint
- Waseda University
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Tennessee Titans: Owner: Amy Adams Strunk. Strunk herself hasnt personally offered a statement, but before the protest policy was put on hold, WKRN reported that head coach Mike Vrabel said that if Titans players decide to stay inside during the national anthem they have Strunks full support. He said, "I told them this morning they had the entire organizations and Miss Amys support to make a decision when that time came." No Titans player has taken a knee and the team has not addressed how it will respond should a player decide to protest on the field.. AFC West. Kansas City Chiefs. Owner: Clark Hunt. Last year, before a game with the Cowboys in November Clark Hunt said, "When it rolled around last year, it really wasnt a big deal for us, and weve tried to stay with that this year. Obviously weve had some guys who have sat or knelt during some of the games this year, but weve continued to work with them and communicate with them that we prefer for them to stand. But at the end of the ...
Molecular Imaging Probes for Diagnosis and Therapy Evaluation of Breast Cancer
F-18 radiolabeled cyclofenil analogues were investigated for imaging of ER-positive breast tumors with PET [32, 33]. C3 site of ... J. W. Seo, J. S. Comninos, D. Y. Chi, D. W. Kim, K. E. Carlson, and J. A. Katzenellenbogen, "Fluorine-substituted cyclofenil ... cyclofenil analogues is more tolerant of steric bulk and polar groups than the C4 site according to the binding affinity to ...
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Clomiphene3
- There are drugs similar to clomiphene that can be taken instead, including tamoxifen and cyclofenil. (essentialparent.com)
- The drugs clomiphene (clomifene), tamoxifen and cyclofenil are used to treat infertility due to failure to produce ova. (thefreedictionary.com)
- HCG is not the perfect hormone to combat Testosterone suppression, and it is used most often in conjunction with estrogen antagonists such as Clomiphene , Tamoxifen or Cyclofenil. (1steroids.net)
Clomid4
- This of course is also the function of Clomid and cyclofenil. (bodybuilding.net)
- The action is similar to Clomid and cyclofenil. (steroizi.ro)
- This is very similar to the function of Clomid® and cyclofenil. (anabolic.org)
- This of breast is gyno not the effectiveness restroom of clomid and cyclofenil. (irtto.com)
Clomifene1
- Cyclofenil is a nonsteroidal SERM and is closely related structurally to triphenylethylene SERMs like clomifene and tamoxifen. (wikipedia.org)
Ovulation2
- Cyclofenil, sold under the brand name Sexovid among others, is a selective estrogen receptor modulator (SERM) medication which is used as a gonadotropin stimulant or ovulation inducer and in menopausal hormone therapy in women. (wikipedia.org)
- Cyclofenil, which is a selective estrogen receptor modulator (SERM) and has been used clinically as an ovulation-inducing drug, showed an inhibitory effect on DENV replication in mammalian cells but not in mosquito cells. (elsevier.com)
Estrogen Receptors3
- Cyclofenil is a SERM, or a mixed agonist and antagonist of the estrogen receptors (ERs). (wikipedia.org)
- Katzenellenbogen, John A. / Fluorine-substituted cyclofenil derivatives as estrogen receptor ligands : Synthesis and structure-affinity relationship study of potential positron emission tomography agents for imaging estrogen receptors in breast cancer . (elsevier.com)
- Similar to the hormone cyclofenil the associated activation of the estrogen receptors is rather low. (anabolicminds.com)
Infertility1
- Cyclofenil is used to treat menstrual disturbances and anovulatory infertility caused by insufficiency of the hypothalamic-pituitary-gonadal axis in women. (wikipedia.org)
SERMs1
- Other SERMs also inhibited DENV replication in mammalian cells, but cyclofenil showed the weakest cytotoxicity among these SERMs. (elsevier.com)
Ondogyne1
- Cyclofenil was first introduced for medical use in 1970 under the brand name Ondogyne in France. (wikipedia.org)
Nolvadex1
- Dat is gyno reduce nolvadex curriculum premenopausal steroid cycle example forum course medication tincidunt en nasal hydrocortisone doeleinden gebruikt kunnen worden. (irtto.com)
Hepatotoxicity1
- Cyclofenil is associated with a relatively high incidence of hepatotoxicity. (wikipedia.org)
Synthesis3
- A time-of-addition assay suggested that cyclofenil may interfere with two stages of the DENV life cycle: the translation-RNA synthesis and assembly-maturation stages. (elsevier.com)
- Novel Selective Estrogen Receptor Ligand Conjugates Incorporating Endoxifen-Combretastatin and Cyclofenil-Combretastatin Hybrid Scaffolds: Synthesis and Biochemical Evaluation. (tcd.ie)
- It is used for the synthesis of raw material for drugs such as cyclofenil, in treating Raynaud's phenomenon in people with scleroderma [ 2 ], and tramadol hydrochloride, that is used for the relief of moderate or severe pain [ 3 ]. (omicsonline.org)
Ligands1
- In a search for estrogen receptor (ER) ligands to be radiolabeled with fluorine-18 for imaging of ER-positive breast tumors with positron emission tomography (PET), we investigated cyclofenil analogues substituted at the C3 or C4 position of the cyclohexyl group. (elsevier.com)
Testosterone3
- Cyclofenil has been used by male athletes to increase testosterone levels. (wikipedia.org)
- In men, cyclofenil can increase testosterone levels due its progonadotropic effects. (wikipedia.org)
- The administration of testosterone-stimulating sub-stances such as HCG, Clornifen citrate or Cyclofenil could be indi-cated since the endogenous testosterone production is considerably reduced by Testosterone heptylate. (steroid.com)
Drugs1
- https://www.drugs.com/international/cyclofenil.html G. Seyffart (6 December 2012). (wikipedia.org)
English1
- Cyclofenil is the English generic name of the drug and its INN, USAN, and BAN. (wikipedia.org)
Treatment2
- Cyclofenil was investigated as a possible treatment for scleroderma in the 1980s, but was found to be ineffective. (wikipedia.org)
- However, the level of intracellular infectious particles decreased more drastically after treatment with cyclofenil than the viral RNA level did, indicating that the assembly-maturation stage might be the main target of cyclofenil. (elsevier.com)
Form1
- Cyclofenil has been available in the form of 100, 200, and 400 mg oral tablets. (wikipedia.org)