Abstract：
:Bioassays were conducted to determine various endocrinological properties of two spirolactone derivatives, 4',5'-dihydrospiro-[estr-4-ene-17,2'(3'H)-furan]-3-one (Compound I) and dispiro[cyclopropane-1,6'-estr-4'-ene-17',2"(3"h)-furan]-3'-one (Compound II). They proved to be very potent estrogen antagonists in immature mice and castrate ewes and neither exhibited inherent estrogenicity. They were moderately active as progestins and gonadotropin inhibitors. Compound II possessed slight androgenic activity and was more active orally than I. Compound I underwent a limited amount of testing in normally cycling rhesus monkeys. It was found to increase viscosity of the cervical mucus and, in oral doses of 0.5 or 2.0 mg/day, prevented pregnancy. One animal given 0.5 mg/day did become pregnant in her first treatment cycle, probably before a drug effect had been established. The results obtained indicate both compounds have potential utility as low-dose oral contraceptives.
journal_name
Steroidsjournal_title
Steroidsauthors
Brooks JR,Steelman SL,Patanelli DJdoi
10.1016/0039-128x(77)90123-4subject
Has Abstractpub_date
1977-06-01 00:00:00pages
809-21issue
6eissn
0039-128Xissn
1878-5867pii
0039-128X(77)90123-4journal_volume
29pub_type
杂志文章相关文献
STEROIDS文献大全abstract：:The 1,3-dipolar cycloaddition of azomethine ylide derived in situ from the reaction of acenaphthylene-1,2-dione and 1,3-thiazolane-4-carboxylic acid to various exocyclic dipolarophiles synthesized from trans-androsterone and trans-dehydroandrosterone afforded a library of novel spiro[5'.2″]acenaphthylene-1″-one-spiro[...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2012.12.017
更新日期：2013-04-01 00:00:00
abstract：:The Na-K-2Cl cotransporter (NKCC2) regulates sodium transport along the thick ascending limb of Henle's loop and is important in control of sodium balance, renal concentrating ability and renin release. To determine if there are sex differences in NKCC2 abundance and/or distribution, and to evaluate the contribution o...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2010.05.014
更新日期：2010-11-01 00:00:00
abstract：:Inhibitors of estrogen 2-hydroxylase can be utilized in studying the kinetics of this cytochrome P450 enzyme complex and in elucidating the structural requirements of the active site. The conversion of estrogens to 2-hydroxyestrogens in rat liver microsomal preparations was examined using two radiotracer assays, the c...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/s0039-128x(83)90120-4
更新日期：1983-07-01 00:00:00
abstract：:The therapeutic use of progesterone following traumatic brain injury has recently entered phase III clinical trials as a means of neuroprotection. Although it has been hypothesized that progesterone protects against calcium overload following excitotoxic shock, the exact mechanisms underlying the beneficial effects of...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2011.02.013
更新日期：2011-08-01 00:00:00
abstract：:Phytochemical characterization of a commercial herb sample supplied as Smilax ornata Lem. (sarsaparilla) led to the isolation of five steroidal saponins, including two new furostanol saponins sarsaparilloside B (1) and sarsaparilloside C (2), whose structures were elucidated via a combination of multistage mass spectr...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2012.01.009
更新日期：2012-04-01 00:00:00
abstract：:In an endeavour to develop potent anti-tumor agents from diosgenin, a series of C-6 derived 1,2,3-triazolyl derivatives were designed and synthesized by employing Cu(I) catalyzed Huisgen 1,3-dipolar cycloaddition reaction of novel azides - (22R,25R)-6β-azidospirostan-3β,5α-diol and 6β-azido-7α-hydroxyspirosta-1,4-dien...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2019.108460
更新日期：2019-11-01 00:00:00
abstract：:Readily available vanadyl acetylacetonate was found to oxidize the allylic sites of Δ(5) steroidal alcohols without protection of hydroxyl groups. Cholesterol, dehydroepiandrosterone, cholesterol benzoate, cholesterol acetate, pregnenolone, and 5-pregnen-3,20-diene were oxidized to 7-keto products using vanadyl acetyl...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2015.06.005
更新日期：2015-09-01 00:00:00
abstract：:The apolar ecdysteroid present in the developing embryo of the blue crab, Callinectes sapidus Rathbun, is tentatively identified as ponasterone A (2 beta, 14 alpha, 20,22-pentahydroxy-5, beta-cholest-7-en-6-one) on the basis of chromatographic, immunological, and mass spectral evidence. The apolar ecdysteroid present ...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(79)90092-8
更新日期：1979-12-01 00:00:00
abstract：:The enterohepatic circulation and metabolism of ethynodiol diacetate (3beta,17beta-diacetoxy-17alpha-ethynyl-estr-4-ene) in baboons were studied following the intravenous injection of this contraceptive steroid labeled with 14C (4-position) and with 3H (in either the 3- or 17-acetoxy moieties). Bile and urine from fou...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(75)90048-3
更新日期：1975-06-01 00:00:00
abstract：:Glucuronidation of 24,25-dihydroxyvitamin D3 has been investigated in in vitro and in vivo experiments. Three positional isomers of 24,25-dihydroxyvitamin D3 monoglucuronide were synthesized from 24,25-dihydroxyprovitamin D3 derivatives with Koenigs-Knorr reaction and used as standard samples. In the presence of the r...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/s0039-128x(99)00057-4
更新日期：1999-10-01 00:00:00
abstract：:Plasma concentrations of dehydroepiandrosterone (DHEA), 5-androstene-3beta,17beta-diol (AED), and 17beta-estradiol (E2) in dairy cows and heifers and AED binding to uterine cytosolic estrogen receptor (ER) were studied. Plasma samples were collected from the subcutaneous abdominal (SA) and jugular (J) veins of heifers...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2003.12.001
更新日期：2004-02-01 00:00:00
abstract：:Synthesis of 7-aryl/allyl-substituted androstene derivatives 3a through 3g has been carried out by Grignard reaction on 3 beta,17 beta-diacetoxyandrost-5-en-7-one (2) with aryl/allyl magnesium bromide. Isomeric mixture of products 3b and 3c/3e and 3f/3h was separated by column chromatography. Stereochemical assignment...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(91)90005-g
更新日期：1991-09-01 00:00:00
abstract：:An homogenate from cortical tissue of mare adrenals was incubated in the presence of tritiated pregnenolone. The (3H) androstenedione and the (3H) testosterone synthesized during the incubation were extracted, purified, and co-crystallized to constant specific activity in the presence of unlabeled carriers. The rate o...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(84)90033-3
更新日期：1984-02-01 00:00:00
abstract：:The inhibition of testosterone 5alpha-reductase activity by 3-oxo-4-androstene-17beta-carboxylic acid in the male reproductive organs of the rat was demonstrated in vitro. The medium for incubation of caput epididymis showed the highest concentration of 5alpha-dihydrotestosterone (5alpha-DHT) whereas the highest conce...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(76)90135-5
更新日期：1976-06-01 00:00:00
abstract：:Based on histological criteria, Kingsley and Bogdanove (3) reported that the benzoate ester of 17beta-hydroxy-5alpha-androstan-3-one (5alpha-DHT), unlike testosterone propionate, is unable to induce vaginal mucification when given subcutaneously to rats. In contrats, Kennedy (4) found in estrogen-pretreated rats that ...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(76)90061-1
更新日期：1976-03-01 00:00:00
abstract：:The role played by progestogens in modulating Schwann cell pathophysiology is well established. Progestogens exert their effects in these cells through both classical genomic and non-genomic mechanisms, the latter mediated by the GABA-A receptor. However, there is evidence that other receptors may be involved. Membran...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2017.09.009
更新日期：2019-02-01 00:00:00
abstract：:The purpose of this study was to determine the short-term effects of progesterone action on estrogen receptor (Re) levels in the rat uterus. Ovariectomized, adrenalectomized rats were maintained on subcutaneous Silastic implants containing crystalline estradiol. Progesterone treatment with serum estradiol maintenance ...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(81)90047-7
更新日期：1981-04-01 00:00:00
abstract：:Bioconversion of the aromatase inhibitor formestane (4-hydroxyandrost-4-ene-3,17-dione) (1) by the fungus Rhizopus oryzae ATCC 11145 resulted in a new minor metabolite 3,5α-dihydroxyandrost-2-ene-4,17-dione (2) and the known 4β,5α-dihydroxyandrostane-4,17-dione (3) as the major product. The structural elucidation and ...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2016.07.003
更新日期：2016-09-01 00:00:00
abstract：:This paper revealed the expression pattern of ERα in the ovoviviparous teleost, Sebastes schlegeli. In this paper, we isolated the cDNA encoding for estrogen receptor alpha of black rockfish (S. schlegeli) from its ovary, named as black rockfish ERα (brfERα). The cDNA sequence of brfERα consists of 2972bp with an open...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2011.09.014
更新日期：2011-12-20 00:00:00
abstract：:Apoptosis is a highly organized mechanism that allows specific cells to die in a controlled manner. Apoptosis can be induced by a variety of agents in a great number of cell types, but cell shrinkage and discrete chromatin cleavage remain common components of apoptosis that is manifested by constitutive enzymes. Despi...
journal_title：Steroids
pub_type： 杂志文章,评审
doi：10.1016/s0039-128x(99)00034-3
更新日期：1999-09-01 00:00:00
abstract：:15alpha-Hydroxydehydroisoandrosterone and 15alpha-hydroxypregnenolone were isolated from hydrolyzed extracts of human late pregnancy urine and identified by means of the isotope dilution technique. In two separate determinations the excretion rate of 15alpha-hydroxydehydroisoandrosterone was found to be 1.7 and 3.2 mi...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/s0039-128x(78)80002-6
更新日期：1978-05-01 00:00:00
abstract：:Dehydroepiandrosterone (DHEA) supplementation has been anecdotally considered as a tool to improve body composition and health status. We aimed to verify the impact of DHEA supplementation on traditional measurements of body composition and blood pressure (BP) due to their clinical applicability. A meta-analysis of ra...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2020.108710
更新日期：2020-11-01 00:00:00
abstract：:This study aimed to develop a quantitative and in vivo magnetic resonance imaging (MRI) approach to investigate the muscle growth effects of anabolic steroids. A protocol of MRI acquisition on a standard clinical 1.5 T scanner and quantitative image analysis was established and employed to measure the individual muscl...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2007.12.011
更新日期：2008-04-01 00:00:00
abstract：:The crystal structures of chenodeoxycholic acid (CDCA), ursodeoxycholic acid (7beta isomer of CDCA) and their other two epimers (3beta,7alpha- and 3beta,7beta-isomers) have been resolved. The four isomers were recrystallized from p-xylene. CDCA crystal is hexagonal P6(5) while the crystals of the other three isomers a...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2007.03.007
更新日期：2007-06-01 00:00:00
abstract：:Agave plants are popular for their myriad applications in traditional medicine attributed to their reported anti-inflammatory, immunomodulatory, cytotoxic and antifungal activities. The aim of this study was to examine the anti-inflammatory, immunomodulatory and ulceroprotective activity of Agave species in relation t...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2020.108648
更新日期：2020-08-01 00:00:00
abstract：:Two new sterols, (24E)-24-n-propylidenecholesterol and 24 epsilon-n-propylcholesterol, were isolated from a cultured marine Chrysophyte. Since most of the steroids found in marine invertebrates are unchanged or modified sterols of algal or symbiotic origin, the discovery of these two unusual sterols in a unicellular a...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(80)90104-x
更新日期：1980-02-01 00:00:00
abstract：:Morphologic changes at the interface of rat endometrial luminal epithelial cells and the stromal cells immediately adjacent were examined and correlated with hypertrophy of the epithelial cells during estradiol (E2) infusion (1 microgram E2/24 h). While the lamina densa in castrate endometrium was thread-like, it beca...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(91)90061-y
更新日期：1991-03-01 00:00:00
abstract：:The isolated perfused rat kidney allows a simultaneous kinetic study of both the renal metabolism and the urinary excretion of cortisol and its metabolites in the rat. In this system, cortisol was completely metabolized within 120 minutes. The main renal metabolites of cortisol (cortisone, 20 reduced cortisol and 20 r...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(77)90052-6
更新日期：1977-11-01 00:00:00
abstract：:The mode of action of steroid hormones has been extended in recent years. In addition to their classical nuclear action (acting as transcription factors), they can also regulate cell-signaling phosphorylation cascades and exert actions that are initiated at the membrane and which, in most cases, are rapid. Even though...
journal_title：Steroids
pub_type： 杂志文章,评审
doi：10.1016/j.steroids.2007.12.009
更新日期：2008-10-01 00:00:00
abstract：:The leaky heme mutants G204, G216, and G214 are shown to accumulate exogenous sterols. Unlike hem mutants which have complete blocks in the heme pathway, these strains do not require ergosterol, methionine, or unsaturated fatty acids for growth. The addition of aminolevulinic acid to the growth medium inhibited sterol...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(89)90035-4
更新日期：1989-03-01 00:00:00
