Algestone
Accumulation and mobilization of triglycerides and cholesteryl esters in Leydig tumor cells. (1/5)
Incubating MA-10 Leydig tumor cells with sodium oleate led to the accumulation of triglyceride within the cells. Triglycerides were deposited in a time- and dose-dependent fashion. Cellular triglyceride promoted storage of cholesteryl ester. As much cholesteryl ester was stored in oleate-treated cells as in cells treated with saturating concentrations of low density lipoprotein. Addition of both oleate and low density lipoprotein resulted in additive accumulation of cholesteryl esters. Cholesteryl esters in cells loaded with triglyceride by oleate treatment were mobilized in response to dibutyryl-cAMP to an extent similar to that in cells containing low triglyceride concentrations. Dibutyryl-cAMP stimulated cholesteryl ester mobilization under all conditions, and stimulated triglyceride mobilization when adequate fatty acid acceptors were available. The results indicate that while triglyceride accumulation in MA-10 cells promoted cholesteryl ester deposition, it did not impair cAMP-dependent cholesteryl ester hydrolysis or steroid hormone production. (+info)Failure of two progesterone antagonists, mifepristone and onapristone, to affect luteal activity in lactating rats. (2/5)
The progesterone antagonists, mifepristone (RU-38,486) and onapristone (ZK-98,299), given as 2 mg daily, did not markedly affect lactation in rats. Both litter growth and time spent by 10-pup litters attached to their mothers were similar in antagonist-treated mothers and in solvent-treated controls. The progesterone antagonists did not affect the steroid content in corpora lutea remaining from the preceding pregnancy. Corpora lutea formed after post-partum ovulation also showed nearly normal function throughout the first 17 days of lactation. It is concluded that progesterone itself plays no role in the initiation or maintenance of luteal function when prolactin secretion is governed through an action independent of the ovaries, as through suckling. Antagonist-treated rats ovulated around Day 13 of lactation despite suckling. This ovulation was not associated with a decrease of progesterone production by the corpora lutea formed after post-partum ovulation. Apparently, elimination of progesterone action may protect corpora lutea from luteolysis. The latter finding indicates a possible role of progesterone in luteolysis and deserves further analysis. (+info)Role of actin in the responses of adrenal cells to ACTH and cyclic AMP: inhibition by DNase I. (3/5)
Erythrocyte ghosts were loaded with pancreatic DNase I and fused with Y-1 adrenal tumor cells to test the possibility that this enzyme might inhibit the steroidogenic responses of the cells to ACTH and cyclic AMP. Fusion of erythrocyte ghosts loaded with DNase I, but not those containing albumin, ovalbumin, boiled DNase I, or DNase I with excess G-actin, inhibited the increase in production of 20 alpha-dihydroprogesterone produced by ACTH and dibutyryl cyclic AMP; inhibition was concentration-dependent with 50% inhibition by 3 X 10(7) molecules of DNase I per cell. It was found that inhibition by DNase I was exerted at the step in the steroidogenic pathway at which cholesterol is transported to mitochondria where steroidogenesis begins. This was shown by measuring transport of cholesterol into the inner mitochondrial membrane, by measuring the production of pregnenolone by isolated mitochondria and by demonstrating that DNase I was without effect on the conversion of pregnenolone to 20 alpha-dihydroprogesterone (an end-product of steroid synthesis). The actin content of Y-1 cells was measured by two methods based upon inhibition of DNase I and by SDS gels following centrifugation. The cells were found to contain 2-3 X 10(7) molecules of actin per cell of which two-thirds is present as G-actin. Since DNase I is known to bind to G-actin to give a one to one complex, these and other findings suggest that at least some of the G-actin in the cells may be necessary for the steroidogenic responses to ACTH and cyclic AMP. (+info)In vivo and in vitro production of progestins by the corpus luteum of pregnancy of the hamster. (4/5)
Synthesis by hamster corpora lutea (CL) in vitro and serum levels of progesterone (P4), 17 alpha-hydroxyprogesterone (17OHP) and 20 alpha-dihydroprogesterone (20DHP) were assessed for different days of pregnancy (Day 1=day of sperm; Day 16=day of delivery). Highest serum levels of the progestins were observed on Day 14 (P4=33 ng/ml; 17OHP=2 ng/ml; 20DHP=3 ng/ml), followed by precipitous declines on Day 16. The highest in vitro levels of luteal P4 and 17OHP were attained on Days 2-6 (production rates of P4=9-30 ng/mg CL/h; 17OHP=0.6-1.5 ng/mg CL/h), and dropped gradually thereafter. In contrast, the production rate of luteal 20DHP was extremely low on Days 2-8 but abruptly increased on Day 10 and was maintained through Day 14 (4-8 ng/mg CL/h). The in vitro production rates of all 3 progestins dropped abruptly on Day 16. Thus, in the pregnant hamster on the day of parturition (Day 16) there was good agreement between in vivo and in vitro levels of the progestins, contrary to the situation in the rat, where on Day 22 the CL in vitro produce large quantities of P4 and 20DHP while the serum levels are very low (Taya and Greenwald, 1981). Addition of 25 ng/ml of ovine LH to the incubation media containing hamster CL increased production rates of P4 (18-55 ng/mg CL/h) and 17OHP (1.5-2.4 ng/mg CL/h) on Days 2, 4 and 14 of pregnancy but the CL were refractory to this dose of LH from Days 6 to 12. The production rate of luteal 20DHP ws never stimulated by the addition of 25 ng LH. These results indicate that P4 is the principal progestin in the pregnant hamster with 17OHP and 20DHP as minor metabolites. The latter 2 progestins have been measured for the first time in the pregnant hamster and the levels are very low in comparison to the pregnant rat. (+info)Effects of peripheral-type benzodiazepine receptor antisense knockout on MA-10 Leydig cell proliferation and steroidogenesis. (5/5)
The peripheral-type benzodiazepine receptor (PBR) is not only widely expressed throughout the body, but it is also genetically conserved from bacteria to humans. Many functions have been attributed to it, but its primary role remains a puzzle. In the current study, we stably transfected cultures of MA-10 Leydig cells with either control or 18-kDa PBR antisense knockout plasmids. The antisense knockout vector was driven by the human enkephalin promoter, which contains two cAMP response elements, such that cAMP treatment of transfected cells could superinduce 18-kDa PBR antisense RNA transcription and, hence, down-regulate endogenous 18-kDa PBR mRNA levels. Control and knockout MA-10 cell lines were then compared at the level of receptor binding, thymidine incorporation, and steroid biosynthesis. Eighteen-kilodalton PBR knockout reduced the maximal binding capacity of tritium-labeled PBR ligands, and the affinity of receptors to the ligands remained unaltered. Additionally, 24-h accumulation of progesterone was lower in the knockout cells. Exposure of the two cell types to 8-bromo-cAMP resulted in a robust increase in steroid production. However, a complex pattern of steroid accumulation was observed, in which further progestin metabolism was indicated. The later decline in accumulated progesterone as well as the synthesis of androstenedione were different in the two cell types. At the level of cell proliferation, reduction of 18-kDa PBR mRNA showed no effect. Thus, we conclude that the 18-kDa PBR may have a more important role in steroidogenesis than in proliferation in this Leydig cell line. (+info)
Algestone
Closely related analogues of algestone include 16α-hydroxyprogesterone, algestone acetonide, and algestone acetophenide. ... Another progestin, algestone acetophenide, in contrast, has been marketed as a hormonal contraceptive. Algestone, also known as ... Algestone (INN), also known as alphasone or alfasone, as well as dihydroxyprogesterone, is a progestin which was never marketed ...
Algestone acetonide
... (developmental code name W-3395), also known as algestone 16α,17α-acetonide or 16α,17α- ... It is the acetonide cyclic ketal of algestone. Another progestin, algestone acetophenide, in contrast, has been marketed. Elks ...
Algestone acetophenide
Estradiol enantate/algestone acetophenide Estradiol benzoate butyrate/algestone acetophenide Sang GW (April 1994). " ... Algestone acetophenide are the English generic name of the drug and its INNM and USAN, while dihydroxyprogesterone acetophenide ... Algestone acetophenide, also known more commonly as dihydroxyprogesterone acetophenide (DHPA) and sold under the brand names ... ISBN 978-3-05-500156-7. Algestone acetophenide, Alphasone acetophenide, Bovitrol, Deladroxone, Dihydroxyprogesterone ...
List of progestogen esters
Algestone acetonide (dihydroxyprogesterone acetonide; 16α,17α-isopropylidenedioxyprogesterone; W-3395) Algestone acetophenide ( ...
Estradiol (medication)
... estradiol enantate with algestone acetophenide as Deladroxate and Topasel; and estradiol benzoate is marketed with progesterone ...
Estradiol enantate
... /algestone acetophenide Estradiol/estradiol enanthate Jarquín González JD, Elda de Aguirre L, Rodríguez C, ... It is formulated in combination with dihydroxyprogesterone acetophenide (DHPA; algestone acetophenide), a progestin, and is ...
Estradiol benzoate butyrate
The combination of EBB and DHPA contains 10 mg estradiol benzoate butyrate (EBB), an estrogen, and 150 mg algestone ... It is formulated in combination with dihydroxyprogesterone acetophenide (DHPA; algestone acetophenide), a progestin, and is ...
Acetophenide
In pharmaceutical chemistry, it is present in algestone acetophenide (dihydroxyprogesterone acetophenide) and amcinafide ( ...
Gestadienol acetate
Analogues of gestadienol acetate include algestone acetophenide (dihydroxyprogesterone acetophenide), demegestone, gestonorone ...
16α-Hydroxyprogesterone
5α-Dihydroprogesterone 11-Deoxycorticosterone (21-hydroxyprogesterone) 20-Dihydroprogesterone Algestone (16α,17α- ...
Mile (band)
... and mixed by noted engineer Chris Lord-Alge (Stone Temple Pilots, Seether, 3 Doors Down). The album was greeted with mixed, ...
C24H34O4
The molecular formula C24H34O4 may refer to: Algestone acetonide Bufalin Medroxyprogesterone acetate Proligestone Testosterone ...
List of drugs: Al
... algestone (INN) alglucerase (INN) alglucosidase alfa (USAN) alibendol (INN) alicaforsen (INN, USAN) aliconazole (INN) ...
Gestonorone caproate
Analogues and derivatives of gestonorone caproate include algestone acetophenide (dihydroxyprogesterone acetophenide), ...
List of progestogens available in the United States
... approved specifically for the treatment of painful endometriosis Acetomepregenol Algestone acetophenide Allylestrenol ...
Hydroxyprogesterone caproate
Analogues of OHPC include other 17α-hydroxyprogesterone derivatives such as algestone acetophenide (dihydroxyprogesterone ...
List of corticosteroid cyclic ketals
Algestone acetophenide (dihydroxyprogesterone acetophenide) Amcinafide (triamcinolone acetophenide) Acroleinides (cyclic ketals ...
Combined injectable birth control
Progesterone derivatives including medroxyprogesterone acetate, algestone acetophenide (dihydroxyprogesterone acetophenide), ... and the second CIC to be studied was estradiol enantate/algestone acetophenide (E2-EN/DHPA) in 1964. In 1967, E2-EN/DHPA was in ... algestone acetophenide 75 to 200 mg in an oil solution The half-progestin-dose formulation of estradiol valerate/norethisterone ... algestone acetophenide (dihydroxyprogesterone acetophenide), hydroxyprogesterone caproate, and megestrol acetate. Estradiol ...
Progestogen-only injectable contraceptive
... have been studied for potential use as POICs but were never marketed as such include the progesterone derivatives algestone ...
List of combined sex-hormonal preparations
2) Estradiol benzoate/estradiol valerate/hydroxyprogesterone caproate (Sin-Ol) Estradiol benzoate butyrate/algestone ... Estradiol enanthate/algestone acetophenide (Anafertin, Deladroxate, Perlutan, Topasel, Yectames) Estradiol valerate/ ...
C29H36O4
The molecular formula C29H36O4 (molar mass: 448.59 g/mol, exact mass: 448.2614 u) may refer to: Algestone acetophenide, or ...
Listen
... a brand name of estradiol enanthate/algestone acetophenide, a form of birth control Listen (horse) (foaled 2005), Irish ...
C21H30O4
The molecular formula C21H30O4 (molar mass: 346.46 g/mol, exact mass: 346.2144 u) may refer to: Algestone, a pregnane steroid ...
List of MeSH codes (D04)
... algestone MeSH D04.808.745.745.654.829.025.025 - algestone acetophenide MeSH D04.808.745.745.654.829.100 - 20-alpha- ...
MeSH Browser
use ALGESTONE to search ALPHASONE 1974-90; use ALGESTONE to search DIHYDROXYPROGESTERONE 1977-present & use ALGESTONE ... Algestone [D04.210.500.745.745.654.829.025] * Algestone Acetophenide [D04.210.500.745.745.654.829.025.025] ... 91(75); was ALPHASONE see under ALGESTONE ACETOPHENIDE/analogs & derivatives 1975-90; was ALPHASONE see under ALGESTONE ... 91; was ALPHASONE see under ALGESTONE ACETOPHENIDE/analogs & derivatives 1975-90; was ALPHASONE see under ALGESTONE ...
DeCS
use ALGESTONE to search ALPHASONE 1974-90; use ALGESTONE to search DIHYDROXYPROGESTERONE 1977-present & use ALGESTONE ... 91(75); was ALPHASONE see under ALGESTONE ACETOPHENIDE/analogs & derivatives 1975-90; was ALPHASONE see under ALGESTONE ... 91; was ALPHASONE see under ALGESTONE ACETOPHENIDE/analogs & derivatives 1975-90; was ALPHASONE see under ALGESTONE ... Algestone - Preferred Concept UI. M0000801. Scope note. A synthetic progestational dihydroxy derivative of PROGESTERONE. Its ...
MH DELETED MN ADDED MN
MeSH Browser
use ALGESTONE to search ALPHASONE 1974-90; use ALGESTONE to search DIHYDROXYPROGESTERONE 1977-present & use ALGESTONE ... Algestone [D04.210.500.745.745.654.829.025] * Algestone Acetophenide [D04.210.500.745.745.654.829.025.025] ... 91(75); was ALPHASONE see under ALGESTONE ACETOPHENIDE/analogs & derivatives 1975-90; was ALPHASONE see under ALGESTONE ... 91; was ALPHASONE see under ALGESTONE ACETOPHENIDE/analogs & derivatives 1975-90; was ALPHASONE see under ALGESTONE ...
FDA UNII Code (use for SPL) FDA Preferred Term NCI Concept Code
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