ANABOLIC-ANDROGENIC ACTIVITY OF A-RING MODIFIED ANDROSTANE DERIVATIVES.

1966 ◽  
Vol 53 (4) ◽  
pp. 627-634 ◽  
Author(s):  
E. F. Nutting ◽  
P. D. Klimstra ◽  
R. E. Counsell
Keyword(s):  
Testosterone Propionate ◽  
Levator Ani ◽  
Levator Ani Muscle ◽  
Reference Standard ◽  
Anabolic Activity ◽  
Androgenic Activity ◽  
Keto Derivative ◽  
Relative Potencies ◽  
Independent Parameters ◽  
Androstane Derivatives

ABSTRACT The activity of 33 steroids, injected intramuscularly, was determined in a castrate rat assay utilizing the responses of the seminal vesicle glands and ventral lobe of the prostate glands as independent parameters of androgenicity and the response of the levator ani muscle as an index of anabolic activity. Testosterone propionate was the reference standard. None of the compounds possessed high androgenic or anabolic activity. The myotrophic and average androgenic relative potencies of the 8 most active analogues ranged from 30 to 89% and 3.1 to 39%, respectively. The most active anabolic compound was the 1-dehydro-3-keto derivative of 17α-methyl-5α-androstan-17β-ol while the widest separation between anabolic and androgenic activities, myotrophic to androgenic ratio of 11.3, was obtained with the 2-dehydro-2-formyl derivative. The effect of various modifications of the A-ring on biological activity are outlined in detail.

ANABOLIC-ANDROGENIC ACTIVITY OF A-RING MODIFIED ANDROSTANE DERIVATIVES.

1966 ◽  
Vol 53 (4) ◽  
pp. 635-643 ◽  
Author(s):  
E. F. Nutting ◽  
P. D. Klimstra ◽  
R. E. Counsell
Keyword(s):  
Seminal Vesicle ◽  
Levator Ani ◽  
Ventral Prostate ◽  
Levator Ani Muscle ◽  
Androgenic Activity ◽  
Specific Position ◽  
Oral Activity ◽  
Methyl Derivatives ◽  
Independent Parameters ◽  
Androstane Derivatives

ABSTRACT The oral activity of 34 steroids administered by stomach catheter was evaluated in castrated rats using the weights of the seminal vesicle glands and ventral lobe of the prostate glands as independent parameters of androgenicity and the weight of the levator ani muscle was used as an index of anabolic activity. 17α-Methyltestosterone was used as the reference standard. A study of various modifications of the A-ring revealed that biological activity was consistent with any one of several distinct changes and did not appear to be related to the electron density in any specific position in the A-ring. Nineteen of the steroids were more potent anabolically than the standard and the eight most active analogues had relative myotrophic potencies ranging from 420–1200% and myotrophic to androgenic ratios ranging from 4.1 to 9.3, respectively. Both saturated and unsaturated 17α-methyl derivatives were represented in this latter group. In general, the most potent compounds anabolically were also among the most active androgenically. Estimates of androgenic potency obtained from the seminal vesicle response were similar to those obtained from the ventral prostate response. The most active anabolic compound (1200%) was the 2-dehydro derivative of 17α-methyl-5α-androstan-17β-ol. The widest separation between anabolic and androgenic activities, myotrophic to androgenic ratio of 9.3, was produced with the 2-dehydro-1α-methyl derivative.

scholarly journals Tetrahydrogestrinone induces a genomic signature typical of a potent anabolic steroid

2005 ◽  
Vol 184 (2) ◽  
pp. 427-433 ◽  
Author(s):  
Fernand Labrie ◽  
Van Luu-The ◽  
Ezequiel Calvo ◽  
Céline Martel ◽  
Julie Cloutier ◽  
...  
Keyword(s):  
Anabolic Steroid ◽  
Gastrocnemius Muscle ◽  
Mouse Genome ◽  
Levator Ani ◽  
Levator Ani Muscle ◽  
Muscle Weight ◽  
Mouse Muscle ◽  
Anabolic Activity ◽  
Androgenic Activity

Tetrahydrogestrinone (THG) is a recently identified compound having the greatest impact in the world of sports. In order to obtain a highly accurate and sensitive assessment of the potential anabolic/androgenic activity of THG, we have used microarrays to identify its effect on the expression of practically all the 30 000 genes in the mouse genome and compared it with the effect of dihydrotestosterone (DHT), the most potent natural androgen. Quite remarkably, we found that 671 of the genes modulated by THG in the mouse muscle levator ani are modulated in a similar fashion by DHT, while in the gastrocnemius muscle and prostate, 95 and 939 genes respectively, are modulated in common by the two steroids. On the other hand, THG is more potent than DHT in binding to the androgen receptor, while, under in vivo conditions, THG possesses 20% of the potency of DHT in stimulating prostate, seminal vesicle and levator ani muscle weight in the mouse. The present microarray data provide an extremely precise and unquestionable signature of the androgenic/anabolic activity of THG, an approach which should apply to the analysis of the activity of any anabolic steroid.

scholarly journals Androgenic and Anabolic Activities of Some Newly Synthesized Epiandrosterone and Progesterone Derivatives.

2000 ◽  
Vol 68 (2) ◽  
pp. 141-157 ◽  
Author(s):  
Y. A. Maklad ◽  
M. M. Nosseir
Keyword(s):  
Prostate Gland ◽  
Levator Ani ◽  
The Body ◽  
Ventral Prostate ◽  
Piperidine Ring ◽  
Albino Rats ◽  
Levator Ani Muscle ◽  
Anabolic Activity ◽  
Androgenic Activity ◽  
Derivatives Of

Derivatives of eplandrosterone and progesterone were synthesized. The androgenic and the anabolic activities of some of tlieln were investigated on prepubertal male albino rats of 21 days old by:-i determining tlie weight gain of the body, levator ani muscle, ventral prostate gland, testis, selniilal vesicles, vas deferens and epididymis, ii- estimation of serum luteinizing (LH) hormone, iii- histopatliological examination of the testis and ventral prostate glands. The results from this study showed that the presence of an appended substituted 2- aminopyridine ring at the C- 17 of testosterone gave the maximum androgenic activity, whereas the presence of a substituted piperidine ring fused to ring D of 5 α- androstane exhibited tlie maximum anabolic activity. However, fusion of a pyrazoline moiety with the ring D of 5 α- androstane led to a compound with considerable androgenic and anabolic activity.

PHARMACOLOGICAL PROPERTIES OF NANDROLONE DECANOATE

1960 ◽  
Vol XXXV (III) ◽  
pp. 405-412 ◽  
Author(s):  
J. de Visser ◽  
G. A. Overbeek
Keyword(s):  
Levator Ani ◽  
Female Rats ◽  
High Dose ◽  
Levator Ani Muscle ◽  
List Type ◽  
Pharmacological Properties ◽  
Nandrolone Decanoate ◽  
Anabolic Activity ◽  
Male And Female Rats ◽  
Dose Levels

ABSTRACT 1. The pharmacological properties of nandrolone decanoate (= caprinate), by abbreviation nor-A. D., have been studied. 2. Nor-A. D. has a marked, long-lasting effect on the levator ani muscle of the castrated rat, but it has little activity on the seminal vesicles and prostate. 3. Nor-A. D. displays only weak gonad inhibiting properties in male and female rats. 4. The anti-oestrogenic activity is low. 5. At high dose levels the anabolic activity becomes maximal and the other effects become evident. The same can be expected to occur if injections are administered with too great a frequency. 6. Chronic toxicity studies in rats and dogs demonstrate its lack of toxicity.

EFFECTS OF TESTOSTERONE AND NANDROLONE AND SOME OF THEIR ESTERS ON THE PSEUDOCHOLINESTERASE ACTIVITY IN THE LIVER AND SERUM AND ON THE SEMINAL VESICLE AND LEVATOR ANI MUSCLE OF THE RAT

1970 ◽  
Vol 64 (3) ◽  
pp. 531-540 ◽  
Author(s):  
R. S. Leeuwin ◽  
E. Th. Groenewoud
Keyword(s):  
Enzyme Activity ◽  
Seminal Vesicle ◽  
Testosterone Propionate ◽  
Levator Ani ◽  
Daily Administration ◽  
Male Rats ◽  
Levator Ani Muscle ◽  
Prolonged Administration ◽  
Potent Effect ◽  
T Testosterone

ABSTRACT Testosterone (T), testosterone-propionate (TP), testosterone-phenyl-propionate (TPP), nandrolone (N) (19-nor-testosterone) and nandrolone-phenyl-propionate (NPP) were compared for their effects on the pseudocholinesterase activities in the liver and serum of castrated male rats. In addition changes in the weight of the seminal vesicle and the levator ani muscle were studied. After daily administration of 1 mg of the hormones for ten days, T and TPP showed a more marked depression of the pseudocholinesterase activity and seminal vesicle than the corresponding nor-derivatives. TP and TPP have approximately similar effects, exceeding those of T. On the levator ani N and NPP were more effective than T and TPP. At identical total doses, administration of all hormones with intervals of more than one day, produced less depression of the pseudocholinesterase activity and less seminal vesicle growth than daily administration. The effects on the levator ani were less influenced by varying intervals. At an interval of four days TPP still had a potent effect on the enzyme activity and the seminal vesicle, whereas T was almost without effect. Prolonged administration showed that the effects on the enzyme activity and the seminal vesicle of N and NPP could not reach the maximum effects of T and TPP respectively.

ORAL ANABOLIC:ANDROGENIC EVALUATIONS OF FOUR ANABOLIC STEROIDS

1966 ◽  
Vol 52 (3) ◽  
pp. 489-496 ◽  
Author(s):  
Aaron Arnold ◽  
Gordon O. Potts
Keyword(s):  
Nitrogen Balance ◽  
Anabolic Steroids ◽  
Levator Ani ◽  
Ventral Prostate ◽  
Levator Ani Muscle ◽  
Anabolic Activity ◽  
Clinical Interest

ABSTRACT Four steroids of potential clinical interest were evaluated in rats for anabolic activity by means of nitrogen balance studies and myotrophically for their effect on the growth of the levator ani muscle. The increase in the weight of the ventral prostate was used as an index of their androgenicity. Under these conditions the nitrogen retention:androgenic and myotrophic:androgenic dissociation ratios were: 17α-methyl-4-chloro-testosterone 0.65:0.12 = 5.4 and 0.32:0.12 = 2.7; 17α-methyl-androst-5-ene-3,17-diol 0.70:0.62 = 1.1 and 0.46:0.62 = 0.7; 17α-methyl-19-nortestosterone 4.6:1.1 = 4.2 and 5.8:1.1 = 5.3; and 1-methyl-androst-1-enolone acetate 0.06:0.15 = 0.004 and 0.72:0.15 = 4.8, respectively. While the nitrogen retention:androgenic and myotrophic:androgenic ratios, in general, are of the same order, it should be noted that there was a marked discrepancy between the nitrogen retention:androgenic and the myotrophic:androgenic ratios for 1-methyl-androst-1-enolone acetate.

EFFECTS OF ANDROGENS AND PROLACTIN ON THE RATE OF PRODUCTION AND COMPOSITION OF SEBUM IN HYPOPHYS-ECTOMIZED FEMALE RATS

1970 ◽  
Vol 48 (3) ◽  
pp. 373-378 ◽  
Author(s):  
T. NIKKARI ◽  
M. VALAVAARA
Keyword(s):  
Production Rate ◽  
Testosterone Propionate ◽  
Skin Surface ◽  
Female Rats ◽  
Sebaceous Glands ◽  
Androgenic Activity ◽  
Surface Lipids ◽  
Skin Surface Lipids ◽  
Relative Potencies ◽  
Stimulation Of

SUMMARY The effect of five androgens on the activity of the sebaceous glands of female rats hypophysectomized at 3–4 weeks of age was studied by determining the rate of production and palmitate: stearate ratio of the skin surface lipids. Both of these values reflected the stimulation of the sebaceous glands by androgens, but the palmitate: stearate ratio appeared to be a more sensitive index of low androgenic activity than the production rate. The response of the sebaceous glands to the androgens tested increased in the order (the relative potencies were calculated from the palmitate: stearate ratios): androstenedione, 17; dehydroepiandrosterone, 33; androstanolone, 48; androstanediol, 91; and testosterone propionate, 100. Prolactin did not enhance the stimulation of the sebaceous glands induced by testosterone propionate.

RESPONSE OF THE SUBMANDIBULAR GLAND OF THE CASTRATED MOUSE TO LOCAL AND SYSTEMIC ADMINISTRATION OF STEROIDS

1963 ◽  
Vol 26 (4) ◽  
pp. 517-523 ◽  
Author(s):  
K. BROWN-GRANT ◽  
W. TAYLOR
Keyword(s):  
Submandibular Gland ◽  
Testosterone Propionate ◽  
Anabolic Steroids ◽  
Levator Ani ◽  
Seminal Vesicles ◽  
Systemic Administration ◽  
Levator Ani Muscle ◽  
Submandibular Glands

SUMMARY The effects of testosterone propionate (TP) and of 17α-ethyl-19 nor-testosterone (ENT) on the submandibular glands, levator ani muscles and seminal vesicles of castrated mice have been compared. ENT restores submandibular weight and histology about as well as TP but has less effect on the levator ani muscle and much less effect on the seminal vesicles. Both steroids can act directly on the submandibular gland. It is suggested that the effect on the gland may be an indication of the 'anabolic' rather than the 'androgenic' potency of the steroids, and the possible use of this response for the assay of 'anabolic' steroids is discussed.

RECOVERY OF GONADAL FUNCTION IN MALE RATS TREATED NEONATALLY WITH 17β-OESTRADIOL BENZOATE

1964 ◽  
Vol 47 (2) ◽  
pp. 200-208 ◽  
Author(s):  
Fred A. Kind ◽  
Manuel Maqueo ◽  
A. Folch Pi
Keyword(s):  
Testosterone Propionate ◽  
Levator Ani ◽  
Seminal Vesicles ◽  
Male Rats ◽  
Ventral Prostate ◽  
Levator Ani Muscle ◽  
Gonadal Function ◽  
Gonadal Activity ◽  
Oestradiol Benzoate ◽  
Old Rats

ABSTRACT Groups of five day old rats were injected with 120 or 240 μg of oestradiol benzoate. When examined at the age of fifty days, the animal presented atrophied testes and marked decreases in the weights of ventral prostate, seminal vesicles and levator ani muscle. Treatment with pregnant mare's serum or with testosterone propionate given from day 20 through day 50 fully restored the gonadal activity. The dose of PMS needed to restore spermatogenesis was 10 IU which was given every third day. Testosterone propionate, 1 mg, given daily was equally effective.

EFFECT OF ANDROGENIC AND ANABOLIC COMPOUNDS ON PSEUDOCHOLINESTERASE ACTIVITY IN THE LIVER AND SERUM OF THE RAT

1965 ◽  
Vol 50 (3) ◽  
pp. 391-402 ◽  
Author(s):  
R. S. Leeuwin
Keyword(s):  
Testosterone Propionate ◽  
Anabolic Steroids ◽  
Levator Ani ◽  
Considerable Effect ◽  
Female Rats ◽  
Male Rats ◽  
Levator Ani Muscle ◽  
Male And Female Rats ◽  
Androgenic Anabolic Steroids ◽  
Androgenic Effect

ABSTRACT Immature male and female rats have a similar basal level of pseudocholinesterase activity in the liver and serum. In male rats pseudocholinesterase activity declines sharply with the onset of sexual maturity, between the fourth and the fifth week, after which it remains more or less constant. In female rats, also coinciding with the onset of sexual development, the activity starts to rise between five and six weeks and then increases gradually up to twenty weeks. Castration of male rats results in an increase of the enzyme activity to the basal level, whereas subsequent injection of testosterone-propionate brings about a fall to the level found in adult male rats. Three androgenic/anabolic steroids were compared for their effects on pseudocholinesterase activities in liver and serum of male castrates, viz. testosterone-propionate, testosterone-phenyl-propionate and nor-testosterone-phenyl-propionate, the latter known to possess a relatively high anabolic potency. This was confirmed in our experiments by direct protein determinations in liver and serum and by levator ani muscle/seminal vesicle ratios. At a dose of 1 mg daily for ten days, the former two substances had a similar considerable effect on pseudocholinesterase activity, whereas the effect of the nor-derivative was much smaller. A response similar to that of one milligram of testosterone-propionate was only obtained with 4 mg of the nor-derivative. At that dose level the androgenic effect of the nor-derivative on the seminal vesicles is somewhat less than that of 1 mg testosterone-propionate daily. It is concluded that the cholinesterase activity lowering effect of the compounds investigated is correlated with their androgenic rather than with their anabolic potencies.

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