A Comparison of the Myotrophic and Androgenic Activities of the Phenylpropionates and Decanoates of Testosterone and Nandrolone

Overbeek, G. A.; Visser, J. de

doi:10.1530/acta.0.0380285

Cited by 23 publications

(5 citation statements)

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“…From this it seems justified to assume that the biological activity induced by testosterone and 19-nortestosterone in the BCLA may be related directly with the extent of binding of both steroids in this muscle. Using the levator ani test (Hershberger, Shipley & Meyer, 1953) it is known from the literature (Barnes et al 1954;Holtkamp et al 1955;Overbeek & de Visser, 1961) that 19-nortestosterone has a greater action on the BCLA than does testosterone. This correlates positively with our binding studies, demonstrating a relatively higher affinity of the BCLA receptor for 19-nortestosterone than for testosterone, the affinity ratio being 1-4.…”

Section: Discussionmentioning

confidence: 99%

“…From pharmacological studies (Barnes, Stafford, Guild, Thole & Olson, 1954;Holtkamp, Heming & Mansor, 1955;Overbeek & de Visser, 1961) concerning anabolic and androgenic potencies of various steroids, it is known that 19-nortestosterone stimulates growth of the bulbocavernosus/levator ani muscle (BCLA) to a greater extent than does testosterone, while testosterone acts more upon the prostate. In addition, Liao, Liang, Fang, Castañeda & Shao (1973) found a positive correlation between the receptor binding in the rat prostate in vitro and biological activity in vivo for several synthetic androgens, including 19-nortesto¬ sterone.…”

Section: Introductionmentioning

confidence: 99%

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COMPARISON BETWEEN THE BINDING OF 19-Nortestosterone, 5α-Dihydrotestosterone AND TESTOSTERONE IN RAT PROSTATE AND BULBOCAVERNOSUS/LEVATOR ANI MUSCLE

Krieg¹,

Dennis²,

Voigt³

1976

Journal of Endocrinology

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Specific binding of (3H)19-nortestosterone in the 100000 g cytosol of the rat bulbocavernosus/levator ani muscle (BCLA) and prostate was demonstrated by agargel electrophoresis at low temperature and compared qualitatively and quantitatively with the binding of tritiated testosterone and 5alpha-dihydrotestosterone (5alpha-DHT). Both tissues showed a greater binding affinity for 5alpha-DHT than for 19-nortestosterone, with testosterone binding the least well of the three. The relative binding affinities in the BCLA and prostate were: 19-nortestosterone:testosterone=1-4, 1.-nortestosterone: 5alpha-DHT = 0.7 The differences were statistically significant (P less than 0-02). The concentrations of receptor sites for 5alpha-DHT were 171 +/- 20 (S.D.) fmol/mg prostatic cytosol protein and 24 +/- 4 (S.D.) fmol/mg BCLA cytosol protein. The in-vitro metabolism of the three steroids in both tissues was aldo investigated by thin-layer chromatography. After incubating for 2 h at 0 degrees C the prostate was shown to reduce 26% of the 5alpha-DHT to androstanediols whilst the BCLA showed a 5% conversion. Testosterone was converted by the prostate to 5alpha-DHT (10%) and the androstanediols (6%) whilst the BCLA showed little activity in this respect. Comparing these in-vitro data with in-vivo findings from the literature, in both organs there is a positive correlation of the extent of binding in vitro to the stimulation of growth in vivo, bearing in mind that testosterone is metabolized to 5alpha-DHT in the prostate whilst in the BCLA, 5alpha-reductase is essentially absent.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

COMPARISON BETWEEN THE BINDING OF 19-Nortestosterone, 5α-Dihydrotestosterone AND TESTOSTERONE IN RAT PROSTATE AND BULBOCAVERNOSUS/LEVATOR ANI MUSCLE

Krieg¹,

Dennis²,

Voigt³

1976

Journal of Endocrinology

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“…This dosage was determined based on our previous dose-dependent study (oil-vehicle, therapeutic dose; 0.375 mg/kg, tenfold higher dose; 3.75 mg/kg, 100-fold higher dose; 37.5 mg/kg body weight) that the most prominent changes of hypothalamic biogenic amines were observed in the tenfold higher dose (3.75 mg/kg) group (Tamaki et al 2003a). This drug is a long-acting steroid ester, which is slowly hydrolyzed to supply constant tissue levels of steroid for more than 4 weeks (Overbeek and de Visser 1961). For long-term analysis (5 and 10 weeks), one to three further administrations of AAS were given at 3-weeks intervals.…”

Section: Experimental Groupsmentioning

confidence: 99%

Anabolic-androgenic steroid does not enhance compensatory muscle hypertrophy but significantly diminish muscle damages in the rat surgical ablation model

Tamaki

Uchiyama

Okada

et al. 2009

Histochem Cell Biol

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Cellular responses in the compensatory hypertrophied (plantaris) muscle induced by surgical ablation of synergistic muscles (soleus and gastrocnemius) were determined during 10-week anabolic androgenic steroid (AAS) treatment. Adult Wistar male rats were divided randomly into the Control and Steroid groups, and contralateral surgery was performed. Nandrolone decanoate was administered to the Steroid group. [3H]thymidine and [14C]leucine labeling were used to determine the serial changes in cellular mitotic activity and amino acid uptake. Myogenic cells and cellular responses in blood vessels and nerve fibers were analyzed by immunohistochemistry. Significantly lower cellular mitotic activity associated with lower volume of muscle fiber necrosis was observed in the Steroid group during the first week. However, amino acid uptake and final muscle wet weight gain did not differ between the groups. Marked activation/proliferation of muscular, vascular, and peripheral nerve-related cells was seen with the inflammatory responses in both groups. However, this activation was dependent on the volume of muscle fiber damage and was not preferentially accelerated by AAS loading. These results indicated that AAS loading significantly diminished muscle fiber damages, but they did not accelerate final muscle wet weight gain and activation of myogenic, vascular, and peripheral nerve related cells in the compensatory enlarged muscles.

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“…Nandrolone and its precursors are anabolic androgenic 19-norsteroids synthetized since the 1950s to enhance the myotropic action and reduce the androgenic side effects of testosterone, from which they structurally derive. [1][2][3] Nandrolone, 19-nortestosterone, is a model 19-norsteroid widely studied in clinical situations to treat various catabolic disorders. [4][5][6][7][8][9][10][11][12][13] It is usually administered by intramuscular injection as decanoate or phenyl propionate ester, even if several oral nandrolone prohormones (19-norandrostenedione and 19-norandrostenediol) formulations have been easily accessible for years as dietary supplements and are still freely available on Internet market.…”

Section: Introductionmentioning

confidence: 99%

“…Nandrolone and its precursors are anabolic androgenic 19‐norsteroids synthetized since the 1950s to enhance the myotropic action and reduce the androgenic side effects of testosterone, from which they structurally derive 1–3 . Nandrolone, 19‐nortestosterone, is a model 19‐norsteroid widely studied in clinical situations to treat various catabolic disorders 4–13 .…”

Section: Introductionmentioning

confidence: 99%

Detecting the abuse of 19‐norsteroids in doping controls: A new gas chromatography coupled to isotope ratio mass spectrometry method for the analysis of 19‐norandrosterone and 19‐noretiocholanolone

Iannella

Colamonici

Curcio

et al. 2020

Drug Testing and Analysis

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The detection of 19-norsteroids abuse in doping controls currently relies on the determination of 19-norandrosterone (19-NA) by gas chromatography-tandem mass spectrometry (GC-MS/MS). An additional confirmatory analysis by gas chromatography coupled to isotope ratio mass spectrometry (GC-C-IRMS) is performed on samples showing 19-NA concentrations between 2.5 and 15 ng/ml and not originated from pregnant female athletes or female treated with 19-norethisterone.19-Noretiocholanolone (19-NE) is typically produced to a lesser extent as a secondary metabolite. The aim of this work was to improve the GC-C-IRMS confirmation procedure for the detection of 19-norsteroids misuse. Both 19-NA and 19-NE were analyzed as target compounds (TCs), whereas androsterone (A), pregnanediol (PD), and pregnanetriol (PT) were selected as endogenous reference compounds (ERCs). The method was validated and applied to urine samples collected by three male volunteers after the administration of nandrolone-based formulations.Before the instrumental analysis, urine samples (<25 ml) were hydrolyzed with β-glucuronidase from Escherichia coli and extracted with n-pentane. Compounds of interest were purified through a single (for PT) or double (for 19-NE, 19-NA, A, and PD) liquid chromatographic step, to reduce the background noise and eliminate interferences that could have affect the accuracy of δ 13 C values. The limit of quantification (LOQ) of 2 ng/ml was ensured for both 19-NA and 19-NE. The 19-NE determination could be helpful in case of "unstable" urine samples, in late excretion phases or when coadministration with 5α-reductase inhibitors occur.

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A Comparison of the Myotrophic and Androgenic Activities of the Phenylpropionates and Decanoates of Testosterone and Nandrolone

Cited by 23 publications

References 0 publications

COMPARISON BETWEEN THE BINDING OF 19-Nortestosterone, 5α-Dihydrotestosterone AND TESTOSTERONE IN RAT PROSTATE AND BULBOCAVERNOSUS/LEVATOR ANI MUSCLE

COMPARISON BETWEEN THE BINDING OF 19-Nortestosterone, 5α-Dihydrotestosterone AND TESTOSTERONE IN RAT PROSTATE AND BULBOCAVERNOSUS/LEVATOR ANI MUSCLE

Anabolic-androgenic steroid does not enhance compensatory muscle hypertrophy but significantly diminish muscle damages in the rat surgical ablation model

Detecting the abuse of 19‐norsteroids in doping controls: A new gas chromatography coupled to isotope ratio mass spectrometry method for the analysis of 19‐norandrosterone and 19‐noretiocholanolone

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