PHARMACOLOGICAL PROPERTIES OF NANDROLONE DECANOATE

1960 ◽  
Vol XXXV (III) ◽  
pp. 405-412 ◽  
Author(s):  
J. de Visser ◽  
G. A. Overbeek

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.

1963 ◽  
Vol 42 (4) ◽  
pp. 601-614 ◽  
Author(s):  
K. Ahrén ◽  
A. Arvill ◽  
Ä. Hjalmarson

ABSTRACT Methandrostenolone (17β-hydroxy-17α-methyl-androsta-1,4-dien-3-one) was injected in 4 dose-levels (0.05, 0.5, 2.5 and 5.0 mg daily for 28 days) into castrated male rats, and the response of the mammary glands, the seminal vesicles and the levator ani muscle studied. One dose-level (2.5 mg daily for 28 days) was injected into castrated female rats, and the response of the mammary glands, the vagina and the uterus studied. The main results were as follows: The 0.05 mg dose did not stimulate the seminal vesicles but produced a slight weight increase of the levator ani muscle. The 0.5 mg dose had only a minimal effect on the seminal vesicles but had a much more pronounced effect on the levator ani muscle. The 2 higher doses, however, markedly stimulated both the seminal vesicles and the levator ani muscle. In the mammary glands methandrostenolone produced not only lobule-alveolar development, as do most other androgens, but in addition induced growth and development of the mammary duct system, as found with oestrogenic compounds. The lobule-alveolar development, found after treatment with the various dose-levels of methandrostenolone, quantitatively, more closely followed the growth of the levator ani muscle than the development of the seminal vesicles. In the castrated female rats methandrostenolone stimulated vaginal opening, brought about slight cornification of the vaginal epithelium and caused a marked weight increase of the uterus. These effects cannot be explained solely on the basis of the androgenic activity of this compound, but seem to indicate that methandrostenolone has an oestrogenic activity when injected into castrated rats.


2000 ◽  
Vol 88 (1) ◽  
pp. 26-34 ◽  
Author(s):  
Ghislaine Gayan-Ramirez ◽  
Hélène Rollier ◽  
Frank Vanderhoydonc ◽  
Guido Verhoeven ◽  
Rik Gosselink ◽  
...  

To examine whether concomitant anabolic steroid treatment combined with training might enhance previously observed training effects (A. Bisschop, G. Gayan-Ramirez, H. Rollier, R. Gosselink, R. Dom, V. de Bock, and M. Decramer. Am. J. Respir. Crit. Care Med. 155: 1583–1589, 1997) and whether insulin-like growth factor I (IGF-I) was involved in these changes, male and female rats were submitted to inspiratory muscle training (IMT) for 8 wk (30 min/day, 5 times/wk) and were compared with untrained controls. During the last 5 wk of training, trained rats were divided to receive weekly either low-dose (LD; 1.5 mg/kg) or high-dose (HD; 7.5 mg/kg) nandrolone decanoate or saline for the IMT and control rats. In both sexes, diaphragm muscle mass and contractile properties were unchanged with treatment. In males, HD resulted in decreased diaphragm type I cross-sectional area (−15%; P < 0.05, HD vs. IMT), whereas no changes were observed in females. Finally, an increase in IGF-I mRNA levels was present in HD male (+73%; P < 0.05, HD vs. IMT) and female treated rats [LD (+58%) and HD (+96%) vs. IMT; P < 0.001]. We conclude that administration of nandrolone decanoate did not enhance the previously observed training effects in rat diaphragm, although it increased the IGF-I mRNA expression levels.


1997 ◽  
Vol 82 (4) ◽  
pp. 1112-1118 ◽  
Author(s):  
Anja Bisschop ◽  
Ghislaine Gayan-Ramirez ◽  
Hélène Rollier ◽  
P. N. Richard Dekhuijzen ◽  
René Dom ◽  
...  

Bisschop, Anja, Ghislaine Gayan-Ramirez, Hélène Rollier, P. N. Richard Dekhuijzen, René Dom, Vera de Bock, and Marc Decramer. Effects of nandrolone decanoate on respiratory and peripheral muscles in male and female rats. J. Appl. Physiol. 82(4): 1112–1118, 1997.—Thirty male and 18 female adult rats received weekly an intramuscular injection of either saline (control; C), 1.5 mg/kg (low-dose; LD) nandrolone decanoate or 7.5 mg/kg (high-dose; HD) nandrolone decanoate during 5 wk. Compared with respective C, growth rate was stunted in male HD rats from 2 wk of treatment on, whereas it was enhanced in female LD and HD rats after 1 wk. Mass of all muscles studied varied proportionally to body weight, except for the gastrocnemius (males: 0.49 ± 0.04 vs. C: 0.52 ± 0.03%, not significant; females: 0.17 ± 0.01 vs. C: 0.15 ± 0.01%, P < 0.05). In vitro contractile and fatigue properties of the diaphragm remained unchanged, except for a decrease in twitch kinetics (time to peak tension: C, 21 ± 2; LD, 19 ± 1; HD, 19 ± 2 ms, P < 0.05; half-relaxation time: C, 26 ± 5, LD, 25 ± 5, HD, 23 ± 3 ms, P < 0.01). Histochemistry of the diaphragm and the gastrocnemius revealed a significant increase in type IIx/b dimensions. In the gastrocnemius, type I fiber dimensions also increased. A pair-fed study, including another 24 female rats, showed that the changes in oral food intake only partly accounted for the observed anabolic effects.


1980 ◽  
Vol 66 (2) ◽  
pp. 131-144 ◽  
Author(s):  
José R. Cabral ◽  
Lorenzo Rossi ◽  
Tommaso A. Dragani ◽  
Giuseppe Delia Porta

3-(5-nitro-2-furyl)-imidazo(1,2-α)pyridine was tested for carcinogenicity by long-term administration in the diet to CTM mice at 0.1, 0.2 and 0.4 % dose levels and to Wistar rats at 0.2 and 0.4 % dose levels, and by short-term intraperitoneal injections to suckling BALB/c mice. The compound was a strong carcinogen. In CTM mice it induced carcinomas of the esophagus and forestomach at all dose levels and thymic lymphosarcomas at the two highest doses. In male and female rats, esophagus and forestomach papillomas were observed at all dose levels, whereas esophagus and forestomach carcinomas and kidney tumors were observed only at the high dose. In female rats, an increased incidence of mammary tumors was seen at the high dose. The treatment of BALB/c suckling mice by intraperitoneal injections did not induce a clear carcinogenic response.


1965 ◽  
Vol 50 (3) ◽  
pp. 391-402 ◽  
Author(s):  
R. S. Leeuwin

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.


2018 ◽  
Vol 7 (5) ◽  
pp. 412-418
Author(s):  
Mohd Urooj ◽  
◽  
Mohammad Ahmed Khan ◽  
G. Thejaswini ◽  
Munawwar Husain Kazmi ◽  
...  

Jawarish Shahi (JS) is a compound polyherbal Unani pharmacopoeial formulation indicated for Khafqan (Palpitation), Nafkh-e-Shikam (Flatulence) and Waswas (Insanity; false perception and hallucinations). Jawarish Shahi contains herbs like Halela (Terminalia chebula), Amla (Emblica officinalis), Kishneez (Coriandrum sativum), Elaichi Khurd, (Elettaria cardamomum), and Bed Mushk (Salix caprea). The present study was carried out as per OECD 408 guidance to evaluate 90 days repeated oral dose toxicity in male and female Sprague Dawley rats. The study was performed at dose levels 1028 and 2000 mg/kg bw. No adverse effects were reported with respect to body weight, feed intake, behavior and clinical signs indicative of systemic toxicity. The expected growth pattern was observed in body weight and feed intake as compared to control group at both dose levels in male and female rats. There were few significant alterations with respect to hematology, and clinical biochemistry, however the results were within normal range thus considered toxicologically insignificant. The microscopic examination of different organ/tissue showed that no histopathological changes were observed. The findings of the study showed that No Observed Adverse Effect Level (NOAEL) for JS is greater than 2000 mg/kg body weight


2020 ◽  
Vol 36 (6) ◽  
pp. 399-416
Author(s):  
Nurhayat Barlas ◽  
Emre Göktekin ◽  
Gözde Karabulut

The present study was designed to evaluate the effects of di- n-hexyl phthalate (DHP) and di-cyclohexyl phthalate (DCHP) on endocrine organs in rats. Oil control, 20-, 100-, and 500 mg/kg dose groups were selected and administered to pregnant rats on gestational days 6–19 by oral gavage. The neonatal stages of rats continued until postnatal day 20 and the- juvenile stages of rats continued until postnatal day of 32. The rats were allowed to mature until the neonatal and juvenile stages and there after, they were divided into four groups corresponding to the treatment levels. Body and organ weights were recorded, serum was collected, and thyroid, pancreas, pituitary gland, and adrenal gland were removed. There was a decrease in body weights in the 20- and 500mg/kg DHP and in the 20-mg/kg DCHP dose groups in neonatal male rats. In contrast, for female rats, there was an increase in body weights in the 100-mg/kg DCHP dose group and there was a decrease in body weights in the 500-mg/kg DHP dose group. Body weights were increased at 20 and 500 mg/kg in the DHP-exposed juvenile male rats. Serum thyroid-stimulating hormone (TSH) levels were increased in neonatal male rats, while they were increased in the 100-mg/kg DHP group of neonatal and juvenile female rats. Serum triiodothyronine (T3) levels were increased at the high dose of DHP for neonatal male rats and at the low and high dose levels of DCHP for female rats. Serum thyroxine (T4) levels were increased in neonatal rats for DHP. Also, some histopathological changes were observed in the thyroid, pancreas, adrenal, and pituitary gland. In conclusion, it was shown that DHP and DCHP caused negative effects on T3, T4, and TSH hormone levels.


1966 ◽  
Vol 52 (3) ◽  
pp. 489-496 ◽  
Author(s):  
Aaron Arnold ◽  
Gordon O. Potts

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.


2015 ◽  
Vol 34 (6) ◽  
pp. 514-533
Author(s):  
Lori H. Moilanen ◽  
Bradford D. Bagley ◽  
Daniel C. Hakes ◽  
Esther F. Hope ◽  
Jill E. Reynolds ◽  
...  

HFPO-Amidol (CAS # 75888-49-2) is a new hexafluoropropylene oxide (HFPO)-based intermediate developed as an alternative to longer chain perfluorinated compounds. The repeated-dose toxicity of this material was evaluated in an Organization for Economic Cooperation and Development 422-compliant, 28-day oral exposure study with a concurrent reproductive/developmental toxicity screening test. Wistar rats received doses of 0, 30, 300, or 1000 mg/kg/d by oral gavage. Statistically significant changes in body weight gain of 1000 mg/kg/d females during the postcoitum period were possibly related to treatment but were considered not adverse, given the slight nature of the changes. The lower food consumption of 300 mg/kg/d females during the postcoitum and lactation period was not considered treatment related given the absence of a time- and dose-related trend and because food intake was generally similar to control levels after allowance for body weights. Statistically significant changes in motor activity (total movements and total ambulations) were noted in 1000 mg/kg/d main male and female rats. The changes observed in female rats were considered not treatment related in the absence of a dose–response trend. The higher motor activity of high-dose males was primarily apparent within the first 10 minutes of the 60-minute measurement period and was suggestive of temporary hyperreactivity to a new environment/stimulus. This increased peak motor activity remained present although at an apparent lower magnitude when measured 13 days after withdrawal of treatment. Because the possible toxicological relevance of the temporarily increased motor activity observed in 1000 mg/kg/d males could not be excluded, these changes were considered possibly adverse in nature. No treatment-related or toxicologically relevant effects were noted on the other parental, reproductive, and developmental parameters investigated in this study. The parental systemic no observed adverse effect level (NOAEL) for this study is 300 mg/kg/d (based on increased motor activity in males), while the reproductive and developmental NOAEL is 1000 mg/kg/d.


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