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PubMed1986

Pharmacokinetic properties of testosterone propionate in normal men.

The pharmacokinetic characteristics of testosterone propionate were studied in normal men after a single im dose of 25 mg testosterone propionate-19,19,19-d3. Plasma levels of testosterone propionate-19,19,19-d3, its active metabolite testosterone-19,19,19-d3, and endogenous testosterone were measured by gas chromatography-mass spectrometry. Testosterone propionate-19,19,19-d3 was gradually transferred from the im injection site to the systemic circulation. The plasma levels of testosterone propionate-19,19,19-d3 were maintained at 2-4 ng/ml between 3 and 36 h after administration. Plasma testosterone-19,19,19-d3 levels were maintained above the physiological testosterone level for 48 h, while plasma levels of endogenous testosterone changed little.

Adult↗
PubMed1983

Induction of male sex behavior in pony mares with testosterone propionate.

Two pony mares were administered 150 mg of testosterone propionate every other day for 20 days (ten injections) and every ten days there-after. An additional two mares and one stallion were not treated and served as controls. Testosterone propionate was dissolved in absolute ethanol and administered subcutaneously. Sex behavior tests were conducted 26 and 40 days after the first injection. Control mares exhibited very little male sex behavior. Both testosterone propionatetreated mares, however, exhibited mounting, sniffing, flehmen, biting and vocalization behavior in the presence of an estrous mare. The testosterone propionate-treated mares mounted and bit estrous mares more frequently than the stallion but exhibited less sniffing, flehmen and vocalization behavior in the presence of an estrous mare than the stallion. Testosterone propionate-treated mares and the stallion mounted an estrous mare 23.3 +/- 9.7 seconds and 172.5 +/- 22.5 seconds, respectively, after being introduced into the pen. Mares in estrus were mounted by the testosterone propionate-treated mares and the stallion an average of 4.0 +/- 1.3 and 1.0 +/- 0 times, respectively, during a ten-minute test. None of the non-estrous mares was ever mounted by the testosterone propionate-treated mares. In summary, testosterone propionate induced male sex behavior in intact mares and the testosterone propionate-treated mares effectively detected estrous mares.

Journal Article↗
PubMed1985

Determination of testosterone propionate in human plasma by gas chromatography-mass spectrometry.

A specific, sensitive and accurate quantitative analysis of testosterone propionate in human plasma was developed using gas chromatography-mass spectrometry-selected-ion monitoring. For the calculation of testosterone propionate in plasma, peak height ratios were measured by selected-ion monitoring performed on the molecular ions of the trifluoroacetyl derivative of testosterone propionate (m/z 440) and testosterone propionate-19,19,19-d3 (m/z 443). The sensitivity of the method was judged from the lower limit of the detection of the mass spectrometer which was at 20 pg. The inter-assay coefficients of variation and relative error at a concentration of 1.31 ng/ml of plasma were 5.47% and -2.3%, respectively. The method described was applied to the determination of plasma concentrations of testosterone propionate-19,19,19-d3 following an intramuscular dose of testosterone propionate-19,19,19-d3 in a healthy male volunteer.

Adult↗
PubMed1978

Polyamines and nucleic acids in the mouse kidney induced to growth by testosterone propionate.

Daily injections of testosterone propionate to castrated mice resulted in a striking increase in kidney weight. Renal putrescine rose sharply and the amounts of spermidine were also increased. The activity or ornithine decarboxylase was enhanced to values of more than 1 000 times the control level within a few days of testosterone substitution. A moderate and temporary increase in the activity of the putrescine-activated S-adenosyl-L-methionine decarboxylase was observed. Testosterone injections produced a large increase of renal RNA but only a minor change in DNA. It is apparent that in mice distinct alterations in polyamine metabolism occur during the development of renal hypertrophy induced by testosterone administration.

Adenosylmethionine Decarboxylase↗
PubMed1994

[The Testosterone Propionate Reference Standard (Control 881) of the National Institute of Health Sciences].

Raw testosterone propionate material was tested for preparation of the "Testosterone Propionate Reference Standard (Control 881)". Analytical data obtained were as follows: loss on drying, 0.1%; melting point, 120.6 degrees C; optical rotation [alpha]20D = + 85.4 degrees; ultraviolet spectrum, lambdamax = 241 nm and specific absorbance E 1cm1% (241 nm) = 483; infrared spectrum, the same as that of the NIHS Testosterone Propionate Reference Standard; thin-layer chromatography, no impurities were detected; high-performance liquid chromatography (HPLC), one impurity was detected; assay result, 100.6% by UV spectrophotometry. Based on the above findings, the raw material was authorized as the Testosterone Propionate Reference Standard (Control 881) of the National Institute of Health Sciences.

Chemical Phenomena↗
PubMed1978

Serum estradiol, testosterone and dihydrotestosterone in male monkeys treated with testosterone propionate.

Serum estradiol (E2), testosterone (T) and dihydrotestosterone (DHT) were measured in juvenile (pre-pubertal) male rhesus monkeys injected with either 8 mg or 80 mg of testosterone propionate (TP). After one week, the three steroids were elevated and remained essentially unchanged for the duration of the study. There was little difference in serum E2 or DHT when comparing the two groups of steroid-treated monkeys. In contrast, T levels were consistently greater in the animals given the high dosage of TP.

Animals↗
PubMed1982

Effect of photoperiod on the growth of reproductive organs and on pineal N-acetyltransferase rhythm in male rats treated neonatally with testosterone propionate.

Neonatal administration of testosterone propionate (TP) sensitized male Wistar rats to photoperiodic regulation of reproduction. Testicular, seminal vesicle and prostate weights in 105-day-old TP-treated rats housed under natural photoperiodic conditions were lower during autumn and winter than during spring and summer. The reproductive organ weights in 75-day-old TP-treated rats kept under artificial lighting regimens were smaller under photoperiods shorter than 10 h per day than under photoperiods of 10 h per day or longer. In TP-treated males, pinealectomy prevented the decrease in reproductive organ weights induced by short days. The pineal involvement in the photoperiodic regulation of reproduction might be mediated by the rhythm in melatonin. Under a 8L:16D regimen, when reproductive organ weights were decreased, the period of high night N-acetyltransferase activity, which determines the period of the increased melatonin production, lasted about 1 h longer than under 12L:12D.

Acetyltransferases↗
PubMed1982

Extended Hildebrand solubility approach: testosterone and testosterone propionate in binary solvents.

Solubilities of testosterone and testosterone propionate in binary solvents composed of the inert solvent, cyclohexane, combined with the active solvents, chloroform, octanol, ethyl oleate, and isopropyl myristate, were investigated with the extended Hildebrand solubility approach. Using multiple linear regression, it was possible to obtain fits of the experimental curves for testosterone and testosterone propionate in the various binary solvents and to express these in the form of regression equations. Certain parameters, mainly K and log alpha 2, were employed to define the regions of self-association, nonspecific solvation, specific solvation, and strong solvation or complexation.

Chemistry, Pharmaceutical↗
PubMed1995

Effects of testosterone, testosterone propionate, 17 beta-trenbolone and progesterone on cell transformation and mutagenesis in Syrian hamster embryo cells.

Testosterone, testosterone propionate, 17 beta-trenbolone and progesterone, which represent the main endogenous and synthetic androgens and a progestin, were evaluated for possible cell transformation and genetic effects in Syrian hamster embryo (SHE) cells. Cell growth was reduced by treatment with the steroids at 10-30 micrograms/ml in a dose-related manner. Testosterone and testosterone propionate were less toxic than the other two steroids. Testosterone, testosterone propionate and progesterone induced morphological transformation of SHE cells with similar transformation frequencies. The most potent effects were observed with testosterone propionate, which induced cell transformation at 1-30 micrograms/ml in a dose-related manner. Testosterone and progesterone transformed cells only at the highest dose (30 micrograms/ml). 17 beta-Trenbolone did not induce a statistically significant level of cell transformations at any dose tested (up to 30 micrograms/ml). The transformation frequencies induced by testosterone, testosterone propionate and progesterone were less than one-half that induced by benzo[a]pyrene at 1 microgram/ml. None of these steroids induced significant increases in frequencies of chromosome aberrations or aneuploidy. Gene mutations were not observed for testosterone at the HPRT or Na+/K+ ATPase locus. Because these steroids are also associated with carcinogenic activity in vivo, these in vitro findings provide a model and new insights into the study of the mechanisms of androgen- and progestin-induced cell transformation.

Animals↗
PubMed1992

The effect of testosterone propionate on growth of broiler chickens.

The effects of testosterone propionate (TP) on body weight, tissue percentages of body weight, serum IgM, and rectal temperature (2 h postinjection) of male and female broiler chickens were investigated at 28 and 48 days posthatching. Testosterone propionate was dissolved in sesame oil and was injected at 2 mg/kg of body weight every other day, and controls were treated with sesame oil at similar volume, starting Day 7 posthatching. Administration of TP reduced (P < .05) body weight and percentages of liver, testes, and bursa of Fabricius at 28 and 48 days of age. At 28 and 48 days of age, muscle percentage and comb growth of TP-treated birds increased (P < .05) but ovarian weight was unaffected. Concentrations of IgM in serum of TP-injected birds was unchanged at Day 28, but increased (P < .05) at Day 48. Testosterone propionate did not affect percentages of bone or abdominal fat in either sex. Rectal temperature was depressed (P < .05) by TP treatment in both sexes at both ages.

Animals↗
PubMed1982

Steroid levels after intramuscular injection of testosterone propionate in the caprine.

Nine sexually mature intact grade does were injected intramuscularly with testosterone propionate and subsequent plasma steroid concentrations determined and male-like behavior recorded. The does received either 100 mg testosterone propionate every three days for six treatments, total dose 600 mg (N = 5); 50 mg testosterone propionate daily for eighteen days, total dose 900 mg (N = 2) or 10 mg testosterone propionate daily for eighteen days, total dose 180 mg (N = 2). The treatments induced male-like sex behavior, the intensity of which was related to the dose of exogenous testosterone used, the regimen of administration, and the plasma levels of testosterone. Exogenous testosterone treatment had minimal effect on the subsequent reproductive activity of the does.

Animals↗
PubMed2000

Testosterone-propionate impairs the response of the cardiac capillary bed to exercise.

OBJECTIVE: Experimental application of anabolic-androgenic steroids and exercise training induce cardiac hypertrophy. This study quantifies for the first time, on microscopical level, the adaptation of the cardiac capillaries and myocytes to the concomitant application of testosterone-propionate and exercise training. METHODS: Female SPF-NMRI mice were studied over 3 and 6 wk. Experimental groups: (i) sedentary control (C); (ii) exercise (treadmill running, E); (iii) testosterone-propionate (TP); and (iv) testosterone-propionate+exercise (TPE). Morphometric parameters: 1) papillary muscles: capillary density, intercapillary distance, number of capillaries around a myocyte, and minimal myocyte diameter; and 2) left ventricular wall: capillary density and intercapillary distance. RESULTS: Papillary muscle: A striking suppression of the exercise-induced improvement in capillary supply occurs in the testosterone-propionate+exercise groups over 3 and 6 wk. Exercise without drugs increases significantly (P < 0.05) the capillary density, shortens significantly (P < 0.05) the intercapillary distance, whereas it increases the number of capillaries around a myocyte. These alterations are not observed in the testosterone-propionate treated sedentary animals; e.g., capillary density after 6 wk (mean values +/- standard deviation, capillaries x mm(-2)): C: 4272 +/- 287, E: 5411 +/- 758, TP: 4221 +/- 364, and TPE: 3997 +/- 397. Moreover, only in the testosterone-propionate+exercise groups occurs a mild myocyte hypertrophy after both time periods: there is a trend toward hypertrophy (P < 0.1) in comparison with the C groups and a significant hypertrophy (P < 0.05) in comparison with the E groups. CONCLUSIONS: Testosterone-propionate profoundly inhibits the exercise-induced augmented capillarization, whereas (under training conditions) it leads to a mild myocyte hypertrophy. The microvascular impairment could trigger an imbalance between the myocardial oxygen supply and demand, especially during physical exercise.

Animals↗
PubMed1988

Pharmacokinetic studies of testosterone propionate using gas chromatography/mass spectrometry/selected ion monitoring.

A sensitive and accurate method for the quantitative estimation of testosterone propionate in human plasma was developed using gas chromatography/mass spectrometry/selected ion monitoring. The method employing stable isotopically labelled testosterone propionate as tracer was employed to follow the time course of plasma testosterone propionate and its active metabolite testosterone in normal men. Intramuscularly administered (19,19,19-2H3)testosterone propionate was readily transferred from the injection site to systemic circulation. Plasma (19,19,19-2H3)testosterone levels were maintained above the physiological testosterone level for 48 h, while plasma levels of endogenous testosterone changed little.

Adult↗
PubMed1975

Effects of testosterone propionate or dihydrotestosterone propionate on plasma FSH and LH levels in neonatal rats and on sexual differentiation of the brain.

The present study tests the hypothesis that the effects of perinatal androgen administration on the development of the brain are brought about indirectly by a suppression of plasma gonadotropin (GTH) titers. Both castrated male and intact female rats were treated neonatally with 5 alpha-dihydrotestosterone propionate (DHTP) or testosterone propionate (TP) throughout the first ten postnatal days of life and the corresponding effects on neonatal plasma FSH and LH levels and the subsequent ability of the adult to exhibit cyclic GTH release and female sex behavior (lordosis) were determined. In males castrated within 24 h of birth, subcutaneous injections of DHTP (60 or 180 mug per 100 g average body weight) or TP (60 mug/100 g) given on day 2, 4, 6, 8 and 10 reduced plasma levels of FSH and LH as determined by radioimmunoassay 48 h following the first and last injections. However, TP but not DHTP masculinized the development of the regulation of GTH release as mesured by luteinization of subcutaneous ovarian grafts, and also suppressed the ability of adult neonatally castrated male primed with estradiol benzoate and progesterone to display lordosis behavior. In intact females, the same neonatal DHTP and TP injection regime lowered FSH and LH plasma levels following the last injection (day 12), while DHTP lowered LH, but not FSH, following the first injection (day 4). All TP treated females had ovaries devoid of CL by 45 days of age and showed prolonged vaginal cornification. However, DHTP failed to masculinize the pattern of GTH release in females since DHTP-treated females, like oil-treated females, possessed CL(days 45 and 100) and exhibited vaginal cycles (days 80-100). Lordosis quotients of females treated neonatally with DHTP were as high as those of oil-treated females and significantly higher than those of TP-treated females. These results demonstrate that the ability of TP to induce maculine differentiation of the neural regulation of GTH release and female sex behavior does not depend on its ability to depress circulating LH and FSH levels in the neonatal male, or LH levels in the neonatal female rat.

Animals↗
PubMed1979

[Testosterone and dihydrotestosterone radioimmunoassays in Müllerian ducts of control and testosterone propionate injected quail embryos (author's transl)].

Testosterone (T) and dihydrotestosterone (DHT) have been quantitated by means of radioimmunoassay in Müllerian ducts (CM) from control quail embryos (6 to 8-day male and 6 to 15-day female) and from female embryos injected with 50 nanograms of testosterone propionate (PT) on the 8th day. These hormones are demonstrable in undifferentiated CM from 6-day control embryos. In control males although a highly significant decrease of the CM weight occurs during the CM involution, the detected amounts of androgens remain at a constant level. In control females, the right CM shows a slight increase of the androgen content during the rudimentation, i.e. from day 8 on; in the left CM: the highest steroid levels are found on the 6th day; while the CM differentiate, concentrations decrease and become similar to those found in neutral tissues. Given testosterone propionate on day 8 female embryos: right CM: both testosterone and DHT levels highly increase until day 14; the CM of treated embryos contain 8 times as much steroid as control; left CM: testosterone and DHT increase after injection until day 9,5; they slightly decrease between days 9,5 and 12, and then remain constant on day 14. Differences in concentrations are highly significant between CM of control and of PT - injected embryos. It seems that the binding sites of these androgens are more numerous during the involution and that bound testosterone or DHT could take a part in CM regression in male embryos and right CM rudimentation in female embryos.

Animals↗
PubMedDate not supplied

Biphasic effect of testosterone propionate on Sertoli cell secretory function.

When various doses of testosterone propionate (10 to 10,000 mug/day) were given to 21-day-old rats for 10 days a biphasic effect was seen both on testis weight and production of androgen-binding protein (ABP). At low doses (10 to 100 mug testosterone propionate/day) there was a reduction in testis weight as well as ABP content in the epididymis. At higher doses of testosterone propionate, there was a stimulation of both testicular weight and ABP production in spite of suppressed serum FSH and LH levels. These effects of testosterone propionate on Sertoli cell secretory function strongly suggest that the Sertoli cell is a target cell for androgen.

Animals↗
PubMedDate not supplied

Short-term effects of an LHRH-agonist alone or in combination with testosterone propionate or indomethacin on rat testes. Evidence of testosterone independent effects. I.

The treatment of adult male Wistar rats with a LHRH-agonist (lutrelin Wyeth/WY 40972) resulted in severe damage of the seminiferous tubules as well as in remarkable changes of the blood vessels within 24 hours. First striking signs of alterations within the blood vessels were already found 6 hours after the injection of lutrelin: the blood vessels were almost totally filled with leucocytes. Neither the effects on the germinal epithelium nor the effects on the blood vessels were prevented by the simultaneous treatment with 3 mg testosterone propionate (TP). The treatment with indomethacin, however, clearly antagonized both events. The complete inefficiency of TP to overcome the inhibitory effects of lutrelin on the testes does argue against an androgen deficiency as the primary cause. The results obtained with indomethacin strengthen the hypothesis, that the early deleterious effects of LHRH-agonists on the germinal epithelium of the rat are primarily caused by circulatory disturbances in the testes and that prostaglandins may act as mediators.

Animals↗