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.

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.

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.

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 ASSAY OF SUBCUTANEOUSLY INJECTED ANDROGENS IN THE CASTRATED RAT

1963 ◽  
Vol 42 (2) ◽  
pp. 245-253 ◽  
Author(s):  
Ralph I. Dorfman ◽  
Adeline S. Dorfman
Keyword(s):  
Double Bond ◽  
Levator Ani ◽  
Seminal Vesicles ◽  
Ventral Prostate ◽  
Methyl Groups ◽  
Albino Rat ◽  
Once Daily ◽  
Methyl Group ◽  
Assay Procedure ◽  
Androgenic Activity

ABSTRACT An assay procedure using the immature castrated albino rat is described using the weight of the seminal vesicles, ventral prostate, and levator ani as end-points in a ten day assay. The sensitivity was of the order of 0.6 mg of testosterone injected subcutaneously once daily in an aqueous suspending medium. The precision was adequate as judged by the λ values of 0.096 to 0.137 for the seminal vesicles, 0.128 to 0.162 for the ventral prostate, and 0.171 to 0.248 for the levator ani. Activity of testosterone was increased significantly by esterification, by introduction of the 17α-methyl group, and by reduction of the Δ4 double bond to the 5α form. Androgenic activity was decreased significantly by oxidation of the 17β-hydroxy group to the 17-keto group and introduction of methyl groups at the 2α- or 6α-positions.

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.

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 CORTISONE ON THE GROWTH OF THE VENTRAL PROSTATE, THE DORSOLATERAL PROSTATE, THE COAGULATING GLANDS AND THE SEMINAL VESICLES IN CASTRATED ADRENALECTOMIZED AND CASTRATED NON-ADRENALECTOMIZED RATS

1970 ◽  
Vol 64 (4) ◽  
pp. 637-655 ◽  
Author(s):  
Lars-Eric Tisell
Keyword(s):  
Levator Ani ◽  
Reproductive Organs ◽  
Seminal Vesicles ◽  
Present Knowledge ◽  
Ventral Prostate ◽  
Levator Ani Muscle ◽  
Smooth Muscle Tissue ◽  
Histological Changes ◽  
Adrenalectomized Rats ◽  
Stimulation Of

ABSTRACT The growth of the ventral and the dorsolateral prostate, the coagulating glands and the seminal vesicles was studied in cortisone-treated and non-treated castrated non-adrenalectomized and castrated adrenalectomized rats. The cortisone was administered in daily doses of 3 mg or 9 mg for a period of 15 days. Combined castration and adrenalectomy resulted in a greater degree of atrophy of the ventral prostate than castration alone, thus indicating some maintenance effect of the adrenals on the ventral prostate. No differences in the other accessory reproductive organs were demonstrated when comparing non-treated castrated non-adrenalectomized with castrated adrenalectomized rats. Both doses of cortisone stimulated the growth of the dorsolateral prostate, the coagulating glands and the seminal vesicles, but the larger dose resulted in a greater degree of stimulation. Only the larger dose of cortisone gave histological changes in the ventral prostate indicative of a slight stimulating effect. Catabolic or anti-anabolic effects of cortisone as registered by a decrease in body weight and weight of the levator ani muscle did not inhibit the growth stimulating effect of cortisone on the accessory reproductive organs. Cortisone stimulated the growth of both the epithelium and the smooth muscle tissue of the glands. The effect on the different accessory reproductive organs after cortisone administration was contrary to previous studies, which demonstrated the stimulating effects of androgens in the rat, in that the ventral prostate was relatively unstimulated. Possible mechanisms for the stimulation of the growth of the accessory reproductive organs are discussed in the light of our present knowledge of cortisone metabolism and of the secretion in the cortisone-treated rats of hormones which have been found to modify the growth of the accessory reproductive organs.

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