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.

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.

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.

scholarly journals Steroidal Androgens and Nonsteroidal, Tissue-Selective Androgen Receptor Modulator, S-22, Regulate Androgen Receptor Function through Distinct Genomic and Nongenomic Signaling Pathways

2008 ◽  
Vol 22 (11) ◽  
pp. 2448-2465 ◽  
Author(s):  
Ramesh Narayanan ◽  
Christopher C. Coss ◽  
Muralimohan Yepuru ◽  
Jeffrey D. Kearbey ◽  
Duane D. Miller ◽  
...  
Keyword(s):  
Androgen Receptor ◽  
Intracellular Signaling ◽  
Molecular Mechanisms ◽  
Levator Ani ◽  
Reproductive Organs ◽  
Cross Reactivity ◽  
Levator Ani Muscle ◽  
Xenopus Laevis Oocyte ◽  
Muscle Weight

Abstract Androgen receptor (AR) ligands are important for the development and function of several tissues and organs. However, the poor oral bioavailability, pharmacokinetic properties, and receptor cross-reactivity of testosterone, coupled with side effects, place limits on its clinical use. Selective AR modulators (SARMs) elicit anabolic effects in muscle and bone, sparing reproductive organs like the prostate. However, molecular mechanisms underlying the tissue selectivity remain ambiguous. We performed a variety of in vitro studies to compare and define the molecular mechanisms of an aryl propionamide SARM, S-22, as compared with dihydrotestosterone (DHT). Studies indicated that S-22 increased levator ani muscle weight but decreased the size of prostate in rats. Analysis of the upstream intracellular signaling events indicated that S-22 and DHT mediated their actions through distinct pathways. Modulation of these pathways altered the recruitment of AR and its cofactors to the PSA enhancer in a ligand-dependent fashion. In addition, S-22 induced Xenopus laevis oocyte maturation and rapid phosphorylation of several kinases, through pathways distinct from steroids. These studies reveal novel differences in the molecular mechanisms by which S-22, a nonsteroidal SARM, and DHT mediate their pharmacological effects.

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.

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.

Hindlimb Muscle Dissection, Permeabilization, and Respirometry v1

2021 ◽  
Author(s):  
Matthew D. Campbell ◽  
David J. Marcinek
Keyword(s):  
Skeletal Muscle ◽  
Muscle Biopsy ◽  
Mitochondrial Respiration ◽  
Gastrocnemius Muscle ◽  
Muscle Fibers ◽  
Mouse Muscle ◽  
Skeletal Muscle Biopsy ◽  
Cellular Environment ◽  
Permeabilized Muscle

The use of permeabilized muscle fibers (PMF) has emerged as a gold standard for assessing skeletal muscle mitochondrial function. PMF provide an intermediate approach between in vivo strategies and isolated mitochondria that allows the mitochondria to be maintained in close to their native morphology in the myofiber while allowing greater control of substrate and inhibitor concentrations. However, like mitochondrial isolation, the primary drawback to PMF is disruption of the cellular environment during the muscle biopsy and preparation. Despite all the benefits of permeabilized muscle fibers in evaluating mitochondrial respiration and dynamics one of the major drawbacks is increased variability introduced during a muscle biopsy as well as intrinsic variation that exists due to sex and age. This study was designed to evaluate how age, sex, and biopsy preparations affect mitochondrial respiration in extensor digitorum longus, soleus, and gastrocnemius muscle of mice. Here we detail a modified approach to skeletal muscle biopsy of the gastrocnemius muscle of mice focused on maintenance of intact fibers that results in greater overall respiration compared to cut fibers. The improved respiration of intact fibers is sex specific as are some of the changes in mitochondrial respiration with age. This study shows the need for standard practices when measuring mitochondrial respiration in permeabilized muscle and provides a protocol to control for variation introduced during a typical mouse muscle biopsy.

scholarly journals In vivo visualization of the levator ani muscle subdivisions using MR fiber tractography with diffusion tensor imaging

2012 ◽  
Vol 221 (3) ◽  
pp. 221-228 ◽  
Author(s):  
Pascal Rousset ◽  
Vincent Delmas ◽  
Jean-Noël Buy ◽  
Alain Rahmouni ◽  
Dominique Vadrot ◽  
...  
Keyword(s):  
Diffusion Tensor Imaging ◽  
Diffusion Tensor ◽  
Levator Ani ◽  
Levator Ani Muscle ◽  
Fiber Tractography
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