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.

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.

THE EFFECT OF NANDROLONE PHENYLPROPIONATE ON 14C-LEUCINE INCORPORATION INTO MUSCLE PROTEIN IN THE RAT AND RABBIT IN VIVO

1974 ◽  
Vol 76 (2) ◽  
pp. 403-416 ◽  
Author(s):  
P. Bresloff ◽  
P. K. Fox ◽  
A. W. Sim ◽  
J. van der Vies
Keyword(s):  
Anabolic Steroid ◽  
Gastrocnemius Muscle ◽  
Muscle Protein ◽  
Anabolic Steroids ◽  
Levator Ani ◽  
Leucine Incorporation ◽  
Levator Ani Muscle ◽  
Corticosteroid Administration ◽  
Nandrolone Phenylpropionate

ABSTRACT Investigations have been carried out into the incorporation of 14C-leucine into muscle protein of rats and rabbits and its modification by various treatments. Significant decreases in the rate of incorporation of 14C-leucine into protein of the gastrocnemius and levator ani muscles of rats have been observed following hypophysectomy, fasting or treatment with a corticosteroid. In these situations, treatment with an anabolic steroid, nandrolone phenylpropionate, always prevented or reversed the decrease in 14C-leucine incorporation in the levator ani muscle but never in the gastrocnemius muscle. In contrast to the situation in the rat, the decreased incorporation of 14C-leucine in the gastrocnemius muscle of the rabbit following corticosteroid administration could be partially reversed by the anabolic steroid. The results demonstrate that 14C-leucine incorporation into muscle protein in vivo following various experimental treatments may vary markedly not only from one species to another but also from one muscle to another. Great care should be taken in interpreting the effect, or lack of effect, of androgenic/anabolic steroids on the basis of the response of a single muscle.

Direct effect of melatonin on the accessory sexual organs in pinealectomized male rats kept in constant darkness

1982 ◽  
Vol 95 (1) ◽  
pp. 87-94 ◽  
Author(s):  
Kazuhiko Shirama ◽  
Tetsuo Furuya ◽  
Yuji Takeo ◽  
Kiyoshi Shimizu ◽  
Kyutaro Maekawa
Keyword(s):  
Marked Decrease ◽  
Levator Ani ◽  
Tissue Level ◽  
Male Rats ◽  
Ventral Prostate ◽  
Constant Darkness ◽  
Levator Ani Muscle ◽  
Organ Weights ◽  
And Function ◽  
Coagulating Gland

Pinealectomized and sham-pinealectomized male rats were subcutaneously implanted with 2 cm silicone elastomer capsules filled with testosterone or dihydrotestosterone (DHT) and placed in constant darkness (DD) for 50 days. The data revealed that the sham-pinealectomized group treated with testosterone differed from the pinealectomized group, having lower weights of accessory sexual organs and levator ani muscle. Pinealectomy had no effect on organ and muscle weights of DHT-treated animals. Exposure of male rats to DD resulted in a marked decrease in weights of ventral prostate, seminal vesicle, coagulating gland and levator ani muscle and a decrease in plasma DHT levels. However there was no significant reduction in plasma LH, FSH or testosterone. Pinealectomy of the rats exposed to DD resulted in restoration of both DHT levels and accessory sex organ weights. Melatonin implants in pinealectomized males led to an increase in both testosterone and DHT levels, accompanied by a decrease in sexual organ weights. The data indicate that the anti-gonadal effect of the pineal gland cannot be completely mediated by melatonin and that melatonin and some unknown factors can act at the tissue level to reduce the size and function of the affected sexual organs.

THE GROWTH OF THE VENTRAL PROSTATE THE DORSOLATERAL PROSTATE, THE COAGULATING GLANDS AND THE SEMINAL VESICLES IN CASTRATED MALE RATS INJECTED WITH ACTH AND/OR INSULIN

1969 ◽  
Vol 62 (4) ◽  
pp. 694-710 ◽  
Author(s):  
Lars-Eric Tisell ◽  
Lennart Angervall
Keyword(s):  
Morphological Changes ◽  
Levator Ani ◽  
Regular Insulin ◽  
Reproductive Organs ◽  
Seminal Vesicles ◽  
Male Rats ◽  
Ventral Prostate ◽  
Levator Ani Muscle ◽  
Adrenal Steroids ◽  
Protamine Zinc Insulin

ABSTRACT The growth of the ventral and the dorsolateral prostate, the coagulating glands, seminal vesicles and levator ani muscle was studied in castrated male rats after fifteen days of daily injections with ACTH or insulin alone, or in combination. ACTH was given in a dose of 8 IU daily. Insulin was administered in increasing daily doses, i. e. regular insulin up to 8 IU and protamine zinc insulin up to 10 IU. After ACTH treatment there were variable histological signs of stimulation of the dorsolateral prostate, while the other accessory reproductive organs showed no response. Regular insulin produced no quantitative or morphological changes in the accessory reproductive organs, and no morphological signs of increased secretion of the adrenal steroids. Administration of ACTH and regular insulin in combination stimulated the growth of all the accessory reproductive organs. Protamine zinc insulin produced prolonged hypoglycaemia and morphological signs of increase secretion of adrenal steroids, thus the adrenals became enlarged and the thymus atrophic. Protamine zinc insulin stimulated growth of all the accessory reproductive organs, a stimulation which was further accentuated after combination with ACTH. Possible mechanisms for the action of insulin on the male accessory reproductive organs are discussed. The varying response of the different parts of the prostate and the seminal vesicles emphasizes the importance of the simultaneous examination of these organs.

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 Tissue Selectivity of the Anabolic Steroid, 19-Nor-4-Androstenediol-3β,17β-Diol in Male Sprague Dawley Rats: Selective Stimulation of Muscle Mass and Bone Mineral Density Relative to Prostate Mass

Endocrinology ◽  
2007 ◽  
Vol 149 (4) ◽  
pp. 1987-1993 ◽  
Author(s):  
Stephanie T. Page ◽  
Brett T. Marck ◽  
James M. Tolliver ◽  
Alvin M. Matsumoto
Keyword(s):  
Bone Mineral Density ◽  
Anabolic Steroids ◽  
Levator Ani ◽  
Levator Ani Muscle ◽  
Sprague Dawley ◽  
Mineral Density ◽  
Sprague Dawley Rats ◽  
Tissue Selectivity ◽  
Prostate Growth ◽  
Stimulation Of

Stimulation of prostate growth is a major concern with testosterone therapy in older hypogonadal men. As a result, nonsteroidal selective androgen receptor modulators with anabolic activity but less prostate stimulation are being developed. Anabolic steroids might exhibit similar tissue selectivity. We hypothesized the anabolic steroid 19-nor-4-androstenediol-3β,17β-diol (3β,19-NA) would increase muscle, lean body mass (LBM), and bone mineral density (BMD) with little stimulation of prostate growth. Male Sprague Dawley rats were implanted with SILASTIC brand (Dow Corning, Midland, MI) capsules containing 3β,19-NA (4, 8, or 16 cm), dihydrotestosterone (DHT) (8 cm), 19-nortestosterone (16 cm), or four empty capsules after undergoing either a sham operation (intact) or orchidectomy (ORX). Serum gonadotropins, measured after 4, 8, or 24 wk of treatment, were significantly lower in 3β,19-NA-treated vs. untreated, intact, and ORX rats (P < 0.05), and testosterone was lowered by 3β,19-NA-treatment of intact animals. LBM and BMD were assessed after 20 wk, and 4 wk later, rats were killed for levator ani muscle and prostate weights. Compared with ORX rats, 3β,19-NA-treated rats had dose-dependent higher levator ani muscle weights, LBM, and BMD, which were similar to intact and DHT-treated rats at the highest 3β,19-NA dose. In contrast, prostate weights in all 3β,19-NA-treated groups were similar to ORX rats and lower than intact and DHT- and 19-nortestosterone-treated rats even at the highest 3β,19-NA dose. In summary, 3β,19-NA increases muscle and bone mass without significant stimulation of prostate growth, suggesting it may have some properties of a steroidal selective androgen receptor modulator. Anabolic steroids such as 3β,19-NA should be studied further to determine their mechanisms of tissue selectivity and effects in men.

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.

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.

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.

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