Anti-inflammatory Benefits of Androstenetriol (5-androstene-3 beta-7 beta-17 beta-triol, beta AET)


Androstene-3 beta-7 beta-17 beta-triol (AET) represents a key naturally occurring 7-hydroxy dehydroepiandrosterone (DHEA) metabolite. Produced from the adrenal gland, DHEA and its sulfate are the major circulating adrenal steroids in humans. Serum levels peak in young adults, but then steadily decline with age, falling over 80% by age 70. DHEA serves as a precursor of male and female sex hormones. (1, 3, 5, 6)


DHEA demonstrates a plethora of anti-aging properties in rodents, including anti-inflammatory, anti-obesity, anti-diabetic, immune enhancing activities, and opposes certain activities of endogenous glucocorticoids (GC). As the literature grew, DHEA became widely used as an anti-aging, anti-stress dietary supplement. Despite these well-documented activities in animal models, DHEA supplementation in humans has yielded inconclusive results and the value of DHEA replacement in humans is controversial. Such widely different outcomes in rodents and humans have been referred to as ‘the DHEA conundrum’. Moreover, the potential therapeutic use of DHEA is limited by its side effects due to its conversion to sex hormones.


One possibility to explain these discrepancies is that a metabolite(s) of DHEA, rather than DHEA itself, may be necessary for its full action in human physiology. DHEA undergoes extensive conversion and derivatization to multiple products by phase 1 reactions involving the cytochrome P450 system, and studies have shown that these phase 1 products can be more potent than parental DHEA. Phase 1 reactions frequently decline in elderly subjects, and since such subjects have been the major participants in human DHEA treatment studies, it is possible that biologically active metabolites of DHEA were not produced in adequate amounts in previous human studies. It is also possible that qualitative changes in DHEA metabolism between rodents and humans will account for these differences.


DHEA oxidation via the action of the enzyme CYP7B leads to the 7-hydroxy derivatives of C-19 steroids, which are collectively present in low nanomolar concentrations in human circulation and are not readily metabolized to potent androgens or estrogens. Many of the functions initially attributed to DHEA from observations in rodents are now thought to be properties of these oxygenated metabolites, particularly AET.

 

Molecular Structure of Androstenetriol


AET possesses some of the anti-inflammatory and GC-opposing activities that have been attributed to DHEA, but with greater apparent potency. Studies with AET demonstrate it markedly up regulates host immune response, prevents immune suppression, modulates inflammation and improves survival after lethal infections by pathogens and lethal radiation. (1, 3, 5, 6)


AET has been shown to be protective against traumatic shock. Traumatic shock activates the hypothalamic-pituitary-adrenal axis (HPA) to mediate a cascade of defensive mechanisms that often include overwhelming inflammatory response and immunosuppression, which may lead to multiple organ failure. In a relevant traumatic hemorrhagic shock rodent model that applies to both combat and civilian sectors, AET provided a significant protective effect and improved survival. In a murine thermal injury model that includes glucocorticoid-induced osteopenia, AET significantly preserved bone mineral content, restored whole body bone mineral content and bone growth, suggesting reversal of GC-mediated adverse effects.


Since AET is a naturally occurring compound there is no patent protection leaving the door wide open for AET analogue research. Harbor BioSciences, Inc. – http://www.harborbiosciences.com/ (Public, OTC:HRBR – http://www.google.com/finance?q=OTC:HRBR ) is exploring a synthetic derivative of AET for the treatment of diseases with underlying chronic inflammation. HRBR has developed 17alpha-Ethynyl-5-androsten-3beta, 7beta, 17beta-triol (HE3286), a synthetic derivative AET. (1, 2, 4, 7)


Within the past two years, animal model studies of HE3286 successfully demonstrate the treatment of lung inflammation without immune suppression, the reduction of established disease of rheumatoid arthritis, and both glucose-lowering and cholesterol-lowering effects. Harbor BioSciences most ambitious project to date is their recently released data regarding that plasma levels of AET positively correlate with BMI in healthy men and women.(1) These observations suggest a compensatory role for AET in preventing the development of metabolic syndrome and obesity. The AET structural core may provide the basis for novel pharmaceuticals to treat this disease, HE3286. Stay tuned.



1. Auci DL, Ahlem CN, Kennedy MR, Page TM, Reading CL, Frincke JM. A Potential Role for 5-Androstene-3[beta],7[beta],17[beta]-triol in Obesity and Metabolic Syndrome. Obesity. http://www.nature.com/oby/journal/vaop/ncurrent/abs/oby2010204a.html


2. Conrad D, Wang A, Pieters R, et al. HE3286, an oral synthetic steroid, treats lung inflammation in mice without immune suppression. Journal of Inflammation 2010;7(1):52. http://www.journal-inflammation.com/content/7/1/52


3. Loria RM. Antiglucocorticoid function of androstenetriol. Psychoneuroendocrinology 1997;22 Suppl 1:S103-8.


4. Lu M, Patsouris D, Li P, et al. A new antidiabetic compound attenuates inflammation and insulin resistance in Zucker diabetic fatty rats. American Journal of Physiology – Endocrinology And Metabolism 2010;298(5):E1036-E48. http://ajpendo.physiology.org/content/298/5/E1036.full


5. Malik AK, Khaldoyanidi S, Auci DL, et al. 5-androstene-3?,7?,17?-triol (?-AET) Slows Thermal Injury Induced Osteopenia in Mice: Relation to Aging and Osteoporosis. PLoS ONE;5(10):e13566. http://www.plosone.org/article/info:doi/10.1371/journal.pone.0013566


6. Marcu AC, Paccione KE, Barbee RW, et al. Androstenetriol Immunomodulation Improves Survival in a Severe Trauma Hemorrhage Shock Model. The Journal of Trauma 2007;63(3):662-9.


7. Offner H, Firestein GS, Boyle DL, et al. An Orally Bioavailable Synthetic Analog of an Active Dehydroepiandrosterone Metabolite Reduces Established Disease in Rodent Models of Rheumatoid Arthritis. Journal of Pharmacology and Experimental Therapeutics 2009;329(3):1100-9. http://jpet.aspetjournals.org/content/329/3/1100.full


8. Stiles AR, McDonald JG, Bauman DR, Russell DW. CYP7B1: One Cytochrome P450, Two Human Genetic Diseases, and Multiple Physiological Functions. Journal of Biological Chemistry 2009;284(42):28485-9.

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Thou Shall Cut on Gear and Bulk off Cycle

How many times have you heard someone say “I’m going to bulk up while on cycle and cut up once I’m finished?” They are probably under the train of thought that they can eat everything in sight as long as it has protein in it. The trainee is most likely using aromatizing bulking agents for their cycle, which elicits estrogenic body fat accumulation in Alpha-2 enriched adipose sites.

Estrogenic Alpha-2 Receptors Shown Below:

A poorly planned diet disregarding quality calories on top of highly aromatizable compounds is a perfect recipe for looking like a sumo wrestler instead of a bodybuilder! These misinformed individuals typically think that they will magically cut up once they cease their cycle of anabolics. Due to an ignorant nutrition program and a lack of understanding about the way hormones work, they set themselves up for a major disappointment.  Sure they naturally lose excessive water retention from discontinuing the aromatizing compounds and fool themselves into thinking they are on their way to being shredded, but that surely isn’t the case. In fact, they will most likely lose everything they gained on cycle, and perhaps look worse than before starting the cycle. An insufficient recovery, due to excessive calorie cutting and ineffective PCT products will yield a catabolic environment. Deciding to diet down during your post cycle therapy is perhaps the most catastrophic time to do so. You see, when in PCT, your endogenous hormone levels are plummeted and high calories from protein, carbohydrates, and fats are crucial in holding size, and keeping cortisol levels under control.  When you diet during a post cycle therapy phase you are essentially pouring more gas on the catabolic fire. You increase cortisol by reducing calories lower than on cycle, incorporating more cardiovascular training, and opting for lighter weight and higher reps for your weight training.  Please do not make this mistake and throw your muscle gains and money down the toilet, and keep reading to learn a better approach to proper hormone cycling.

——–OR——–

The wisest approach when cycling would be to aim for an extreme composition change where you diet stringently to achieve the lowest body fat possible, while gaining muscle mass in the process. In order to accomplish such a feat, you need to be incredibly meticulous with your diet, training, and cardio regimen.  You should plan a cycle that is safe and effective so you have adequate time to meet your goal. A 12-18 week cycle would be recommended as you want to gradually lower body fat and increase muscle mass. The first half of the cycle and sometimes a little longer is what I refer to as “the grace period,” meaning, at that time you should still have adequate nutrition for muscle accrual yet low enough calories to continuously shed body fat. The final 4 weeks of the diet should be brutally strict and at this time you will you go from “ripped” to “shredded.” Calories are further reduced and cardiovascular exercise is maximized, the exogenous hormones will be able to prevent you from burning up muscle.

“RIPPED to SHREDDED”

——TO——

Once the cycle is concluded you should be in the best shape of your life and looking absolutely amazing with paper thin skin, pronounced vascularity, and very chiseled features. By having the discipline and mental toughness to get yourself into such lean condition, you have set yourself up for a very productive Post Cycle Therapy and mass gaining phase simultaneously. You will need to plan your off cycle and bulking phase to perfection to yield the desired results. I would recommend Human Chorionic Gonatropin to have been sporadically implemented into the cutting cycle to keep luteinizing hormone and follicle stimulating hormone still functioning at some capacity. Proper SERM selection would be ideal for PCT alongside natural hormonal boosters such as, trans-resveratrol, d-aspartic-acid and quality Bulgarian tribulus.

HCG + Sustain Alpha + TCF-1 + Tribestan = Superior Hormonal Recovery.

+ + +

In the initial stages of your post cycle phase you want to really take advantage of your rebound, and voracious appetite, and ingest copious amounts of quality foods. Months of dieting dramatically increases your insulin sensitivity, which makes processing glucose from carbohydrates very efficient, driving nutrients into muscle cells opposed to adipose tissue.  You should prioritize nutritious carbohydrate sources from whole oats, yams, Ezekiel bread, various beans and berries. Fats should be from whole eggs, red meat, and essential fatty acids. Protein should be in ample supply from all sources. The first 2 weeks of this off-cycle and bulking phase will be incredible as you will soak up nutrients like a sponge and muscle cells will be engorged with glycogen, minerals, and amino acids. Strength will be creeping up from the extra weight gain and water retention, while fat accumulation hasn’t started to  manifest itself yet.

Ideal protein sources:                      Ideal carb sources:                    Ideal fat sources:
-Bonesless,skinless chicken breast       -Whole oats                                 -Egg yolks
-Lean and fatty fresh fish                      -Yams                                           -Olive oil
-Cottage cheese                                   -Flourless Breads                         -Fish oil
-Lean cuts of red meat                         -Black beans                                 -Raw nuts
-Whole eggs                                         -Berries                                         -Fat from meat

Keep in mind, what goes up, must come down. Meaning, you cannot keep forcing high calories like the first 3-4 weeks or else you are asking for excessive body fat accumulation. After week 4, you must put on the brakes and begin cycling your carbohydrates and calories accordingly to make sure you stay in acceptable condition for your bulking phase. This cycling practice is very common amongst competitive Bodybuilders who choose to stay natural in the off-season and only use hormonal assistance when preparing for a competition.  This method will allow you to get into amazing condition while on cycle and essentially grow off cycle. You also increase your post cycle recovery by introducing an influx of calories, which will boost insulin and testosterone from the carbohydrate and dietary fat intake.  You also get to give your endocrine system a nice break and clean out, so you can be receptive for your next bout of cycling. By now you should realize how detrimental it is to not diet or “cut up” once you conclude your steroid cycle, and that doing the exact opposite will be your best plan of action in achieving the optimal results for the goal at hand.

References:
1.) Demling RH, Orgill DP. The anticatabolic and wound healing effects of the testosterone analog oxandrolone after severe burn injury.  J Crit Care. 2000 Mar;15(1):12-7.

2.) D’Aniello A, Di Cosmo A, Di Cristo C, Annunziato L, Petrucelli L, Fisher GH:
Involvement of D-aspartic acid in the synthesis of testosterone in rat testes. Life Sci. 1996, 59:97-104.

3.) D’Aniello A, Di Fiore MM, D’Aniello G, Colin FE, Lewis G, Setchell BP: Secretion of
D-aspartic acid by the rat testis and its role in endocrinology of the testis and
spermatogenesis. FEBS Letters 1998, 436:23-27.

4.) Meikle AAW, Stringham JJD, Woodward MMG, McMurry MMP. Effects of a fat-containing meal on sex hormones in men. Metabolism, clinical and experimental 1990;39:943-6.

5.) Ferrando AA, Chinkes DL, Wolf SE, Matin S, Herndon DN, Wolfe RR. 1999 A submaximal dose of insulin promotes net skeletal muscle protein synthesis in patients with severe burns. Ann Surg. 229(1):11–18.

Cynostane

Diagram of molecule

Chemical Name(s):

2-cyano-17a-methyl-17b-hydroxy-androstan-3-one
2-cyano-17a-methyl-17b-hydroxy-androst-3-one (incorrect name)
Chemical Formula: C21H31NO2
Molecular Weight: 329
CAS: NA
Q Qatio: NA
Anabolic #: NA
Androgenic #: NA
Oral Bioavailability: Estimated at 40%
AR Binding Affinity: NA
SHBG Binding Affinity: NA
Half Life: NA
Legal Status (US): Not listed as a controlled substance
Average Dose:
40-50mg/day standalone
20-30mg/day when stacking
Average Cycle Length: 4-6 weeks
Stimulator
Inhibitor

-5
-4
-3
-2
-1

0
1
2
3
4
5

Muscle Gain

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Strength Gain

[][]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Fat Gain (negative indicates fat loss)

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Water Retention (extra-cellular bloat)

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Aggression

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Libido

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Acne

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Hair Loss

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Prostate Enlargement

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Liver Toxicity

[][]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Lethargy

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Characteristics

2-cyano-dromostolone is a 17aa molecule relatively new to the scene with very few reviews as of yet.

It has a cyano group attached to the 2 position. The chemical structure is the same as methyldrostanolone (Superdrol), except it has a CN group on the 2 position instead of a methyl group. It is a C-17aa steroid and it will be liver toxic. Although, due to the lack of the 4-ene on ring A and lack of 2-methylation, liver toxicity may be reduced relative to a di-methylated steroid such as Superdrol.

So far, feedback is very limited for this compound. However results would be expected to be fairly lean as this compound cannot convert to estrogen. Based on the chemical structure the anabolic potency would appear to be fairly potent with moderate androgenic potency.

At the time of this writing there was only one manufacturer to bring this product to the market and there seems to have been a nomenclature mistake on the labeling for this steroid. The chemical name contains the term “androst”, assuming that there is some sort of ene group on ring A. But there does not seem to be such mention of an ene group on ring A. Therefore, the term androst should be androstan. But if this is the case, the 2-cyano group needs to be stated as alpha or beta. This makes a big difference, since usually C2-alpha groups are significantly more effective than beta.

There are studies about other 2-cyano steroids such as 2-cyano-DHT and 2-cyano-progesterone. In separate studies, one done on dogs, it was seen that both of these 2-cyano steroids caused inhibition of 3b-HSD enzyme. This inhibition would cause severe adrenal suppression. This is a very unsafe inhibition. Whether it occurs in this cyano steroid is unknown, but users need to be aware of this possibility.

Common Clones:

Cynostane by Anabolic Innovation


Related Discussion

The Official Cynostane Thread
Posted by Eric

References

Anabolic Pharmacology
Seth Roberts (2009)

1,4,6 Androstatriene-dione (ATD)

Diagram of molecule

Chemical Name(s):

Androsta-1,4,6-triene-3,17-dione
1,4,6-androstatriene-3,17-dione
Chemical Formula: C19H22O2
Molecular Weight: 282
CAS: NA
Q Qatio: NA
Anabolic #: NA
Androgenic #: NA
Oral Bioavailability: Estimated at 4%
AR Binding Affinity: NA
SHBG Binding Affinity: NA
Half Life: 2 days
Legal Status (US): Not listed as a controlled substance
Average Dose: 25-100mg/day
Average Cycle Length: 4-8 weeks
Stimulator
Inhibitor

-5
-4
-3
-2
-1

0
1
2
3
4
5

Muscle Gain

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Strength Gain

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Fat Gain (negative indicates fat loss)

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Water Retention (extra-cellular bloat)

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Aggression

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Libido

[][]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Acne

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Hair Loss

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Prostate Enlargement

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Liver Toxicity

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Lethargy

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Characteristics

ATD is a steroidal aromatase inhibitor, known as a suicidal inhibitor because it permanently binds to the aromatase enzyme.

ATD is used for its aromatase inhibiting and testosterone boosting effect. Its effectiveness at lowering estrogen appears to be stronger than 6-oxo. It converts to 1,4,6-testosterone, which would also be expected to cause falsely high readings for a testosterone analysis.

The 1,4,6-testosterone metabolite of ATD can also bind to the androgen receptor (AR) and induce androgenic (or possibly anti-androgenic) effects similar to what is seen from 6-oxo. This would be expected since 1,4,6-testosterone has about one third the binding affinity for the AR, therefore it may interefere with the anabolic or androgenic action of hormones which bind the androgen receptor.

ATD would also be expected to interfere with production of natural testosterone by acting upon the hypothalamus pituitary testicular axis (HPTA), therefore this compound should not be used during post cycle therapy (PCT), however it could successfully be used during a cycle to help keep estrogen in control. Anecdotal reports and animal studies have also shown ATD inhibits libido and general sexual potency.

Common Clones:

Arom-X by Advanced Muscle Science (AMS)
AIFM by Anafit
ATD MAX by Anabolic Formulations
ATD-JET by Molecular Developments
Reversitol by IForce


Related Discussion

The Official 1,4,6 Androstatriene-dione (ATD) Thread
Posted by Eric

References

Effect of an inhibitor of aromatization, 1,4,6 androstatriene-3,17-dione (ATD) on LH release and steroid binding in hypothalamus of adult female rats.

Exp Brain Res. 1986;64(3):407-10.
Slama A, Gogan F, Sarrieau A, Vial M, Rostene W, Kordon C.

Effects of ATD on male sexual behavior and androgen receptor binding: a reexamination of the aromatization hypothesis.
ME Kaplan and MY McGinnis
Horm Behav, Mar 1989; 23(1): 10-26.

Anabolic Pharmacology
Seth Roberts (2009)

Methylstenbolone

Diagram of molecule

Chemical Name(s):
2,17a-Dimethyl-17b-hydroxy-5a-androst-1-en-3-one
Chemical Formula: C21H32O2
Molecular Weight: 316.5
CAS: NA
Q Qatio: 3.9
Anabolic #: 660
Androgenic #: 170
Oral Bioavailability: Estimated at 50%
AR Binding Affinity: NA
SHBG Binding Affinity: NA
Half Life: NA
Legal Status (US): Not listed as a controlled substance
Average Dose:
5-20mg/day standalone
1-5mg/day when stacked
Average Cycle Length: 2-4 weeks

 

Stimulator
Inhibitor

 

 
-5
-4
-3
-2
-1

0
1
2
3
4
5

Muscle Gain

[][][][][]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Strength Gain

[][][][][]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Fat Gain (negative indicates fat loss)

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Water Retention (extra-cellular bloat)

[][]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Aggression

[][][][]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Libido

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Acne

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Hair Loss

[][][]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Prostate Enlargement

[][][]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Liver Toxicity

[][][][][]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Lethargy

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

 

Characteristics

Although this compound cannot convert to estrogen, it will bind strongly to SHBG, thus increasing freely circulating estrogen (and testosterone). While there is a lack of anecdotal feedback from this compound to tell the real world effect this compound may have on causing gyno, experience with related compounds tell us gyno symptoms may occur.

Users should be very careful with methylstenbolone and start out with a very low dose. This compound will likely produce a rapid increase in intracellular water retention by inhibiting 11-beta hydroxylase and building up levels of mineralcorticoids that will encourage sodium and water retention.

Gains upwards of 20-25lbs in 4 weeks are probably possible with this compound. However the liver toxicity issues would likely be the first reason why someone wouldn’t be able to make incredible gains from this compound. For this reason it would be extremely important to pre-condition the liver with a liver protecting supplement prior to cycling this compound, while continuing use throughout the cycle and during PCT.

The strength increases from this compound will likely encourage weight lifting heavier than tendons and joints are prepared to lift. It is recommended to be cautious of this and to naturally build up strength levels prior to cycling this steroid.

Using a low dose of methylstenbolone with a moderate dose of a non-methylated compound would be an acceptable way to try to limit the side-effects from this compound, although caution would still need to be taken for liver health no matter what dose is used.

Because of the strength and weight gain this compound would offer it would likely be best used as part of a bulking cycle.

Availability: 

UltraDrol by Antaeus Labs

Related Discussion

The Official Methylstenbolone Thread
Posted by Eric

References

Anabolic Pharmacology
Seth Roberts (2009)

Promestanolone

Diagram of molecule

Chemical Name(s):
17a-methyl etioallocholan 17b-ol 3-hydroxyimine
Chemical Formula: C20H33NO2
Molecular Weight: 319.5
CAS: NA
Q Qatio: 2.4
Anabolic #: 380/24
Androgenic #: 158/20
Oral Bioavailability: Estimated at 40%
AR Binding Affinity: NA
SHBG Binding Affinity: High
Half Life: NA
Legal Status (US): Not listed as a controlled substance
Average Dose:
75-100mg/day standalone
50-75mg/day when stacking
Average Cycle Length: 4-6 weeks
Stimulator
Inhibitor

-5
-4
-3
-2
-1

0
1
2
3
4
5

Muscle Gain

[][]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Strength Gain

[][][]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Fat Gain (negative indicates fat loss)

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Water Retention (extra-cellular bloat)

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Aggression

[][]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Libido

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Acne

[][]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Hair Loss

[][][]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Prostate Enlargement

[][][]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Liver Toxicity

[][][]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Lethargy

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Characteristics

Promestanolone is a 17aa pro-steroid which converts to the illegal anabolic steroid methyl-DHT (mestanolone).

There is no human clinical data on promestanolone, but it is most likely exerting its effects by converting to methyl-DHT. The acidic environment in the stomach would be responsible for converting the 3-hydroxyimine group to a 3-one — thus rapidly changing it to methyl DHT. Therefore results and side-effects would be considered to be very similar to methyl-DHT.

Although DHT can be deactivated in skeletal muscle tissue by 3b-HSD it is likely that this enzyme pathway can be overwhelmed if this compound is taken at a high enough dose. Methyl-DHT has some activity on the progestin receptor, but not to a high degree. It has moderate anabolic but high androgenic effects. It binds strongly to SHBG, therefore free testosterone and estrogen can be expected to rise by displacement from SHBG.

Since this is a 17aa compound, liver toxicity will be an issue with high doses or long term use. For this reason users should consider priming the liver with a liver supporting supplement before and during a Promestanolone cycle. Users will also experience minimal subcutaneous water retention since there is no conversion to estrogen. However, intracellular water and sodium retention will increase by inhibition of 11-beta hydroxylase and mineralocorticoid build up.

Users may also experience an increase in aggression and mood swings which is a common side effect of many steroids with high androgenic value. This makes this compound an excellent pre-lifting or pre-competition steroid.

Promestanolone should produce solid lean gains in muscle as a standalone. However for those looking to add additional bulk to their cycle, promestanolone would stack with with virtually any other non-17aa oral.

Common Clones:

D-Plex by Competetive Edge Labs (CEL)
The ONE by Applied Nutraceuticals


Related Discussion

The Official Promestanolone Thread
Posted by Eric

References

“Effect of 1-alkyl substitution on the biological action in a series of androstanes.”

Cekan Z, Pelc B.
Steroids. 1966 Aug;8(2):209-18.

“Relative binding affinity of anabolic-androgenic steroids: comparison of the binding to the androgen receptors in skeletal muscle and in prostate, as well as to sex hormone-binding globulin.”
Saartok T, Dahlberg E, Gustafsson JA.
Endocrinology. 1984 Jun;114(6):2100-6.

norDHEA

Diagram of molecule

Chemical Name(s):

5-estren-3b-ol-17-one
Nordehydroepiandrosterone
Chemical Formula: C18H26O2
Molecular Weight: 274
CAS: NA
Q Qatio: NA
Anabolic #: NA
Androgenic #: NA
Oral Bioavailability: Estimated at 4%
AR Binding Affinity: NA
SHBG Binding Affinity: NA
Half Life: NA
Legal Status (US): Not listed as a controlled substance
Average Dose:
300-600mg/day standalone
200-300mg/day when stacked
Average Cycle Length: 4-6 weeks
Stimulator
Inhibitor

-5
-4
-3
-2
-1

0
1
2
3
4
5

Muscle Gain

[][]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Strength Gain

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Fat Gain (negative indicates fat loss)

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Water Retention (extra-cellular bloat)

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Aggression

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Libido

[][]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Acne

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Hair Loss

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Prostate Enlargement

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Liver Toxicity

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Lethargy

[]
-5
-4
-3
-2
-1

0
1
2
3
4
5

Characteristics

norDHEA is a non-methylated (non-17aa) pro-steroid. (naturally occurring in trace amounts in humans)

norDHEA can convert to the illegal anabolic steroid nandrolone by converting to norandrostenediol/norandrostenedione, and then to nandrolone. Nandrolone is known to have stronger anabolic effects than testosterone, yet weaker androgenic effects.

norDHEA will aromatize to estrogen less than regular DHEA, but because it is a nor compound it lacks strong androgenic metabolites. For instance, after nandrolone interacts with 5a-reductase, the metabolite dihydronandrolone (DHN) is formed, which is a weaker nor-version of DHT.

Ironically, the lack of estrogen conversion from norDHEA is probably balanced by the lack of androgenic potency and progestational effects, which makes the possibility of bloating and experiencing gyno about as likely as with regular DHEA.

One difference between norDHEA and DHEA that should be considered is the fact that norDHEA will have less androgenic effects, which may pose less risk of androgenic related hair loss and/or acne. This may be a smart choice for some men, and a decent choice for women looking for a moderately anabolic compound without much androgenic effect. (to avoid masculinizing side-effects)

Because of the low bio-availability, high doses must be used to notice gains in lean muscle mass and strength. Even with higher doses, the gains will be mild to moderate. Some bloat should be expected from the estrogenic and progestational effects of the nor-steroids. Because this steroid is non-17aa there should be less concern about it negatively affecting the HDL/LDL ratio.

Like the other DHEA derivatives, norDHEA would be useful in a transdermal application since the enzymes needed for the conversions to more powerful metabolites are concentrated in the skin and absorption through the skin using a good transdermal delivery cream could allow for 5-10x higher absorption than oral.

This compound would stack well with almost any other steroid, except those with progestational activity.

Common Clones:

Decavol by Advanced Muscle Science (AMS)


Related Discussion

The Official norDHEA Thread
Posted by Eric

References

Anabolic Pharmacology
Seth Roberts (2009)

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