Printable View
The following posts represent steroid profiles originally released by Henryv on PHF.
©Henryv, All Rights Reserved.
Printed with Permission.
Henry has warned that some of these profiles may be slightly outdated or limited on information.
Please support Henryv by visiting his website: Total Flex Blog
H-Drol
Attachment 157
Nomenclature: 4-chloro-17a-methyl-androst-1,4-diene-3b,17b-diol
Originally brought to market by Gaspari Nutrition as "Halodrol 50", this compound is the diol version of the steroid the East Germans were taking to cheat at the Olympics in the late 60s and early 70s, Oral Turinabol (4-Chlorodehydromethyltestosterone). Basically h-drol is M14ADD with a chlorine atom attached at the 4-position. This 4-chloro group effectively prevents both aromatisation (conversion of the compound to estrogen) meaning that gynecomastia through excess estrogen should not occur, and water retention is not a problem. The 1,4-diene structure prevents 5-a reduction (conversion to a DHT-based steroid), so androgenic effects like hair loss are much less of a concern.
H-drol cycles are typically 75mg each day for six weeks, first time users may find 50mg effective, though those with more experience may try 100mg. Common side effects include high blood pressure and back and shin pumps, and being methylated there is a mild degree of hepatotoxicity.
M1,4add
Attachment 170
Nomenclature: 17a-methyl-1,4-androstadiene-3b,17b-diol or 17a-methyl-androst-1,4-diene-3b,17b-diol
Essentially this is a prohormone to the most popular designer steroid of all time: dianabol. Conversion rates around 15% are usually discussed, though it's likely to be "broscience". Like d-bol, it's 17a-methylated (meaning some degree of liver toxicity is to be expected), and can aromatise to a potent methylated estrogen, which makes gyno a possibility. Water retention is also likely to be an issue, with some of the weight and strength gained on cycle typically lost on cessation.
Cycles are typically 90 - 120mg a day for four to six weeks.
M-lmg
Attachment 169
Nomenclature: 13-ethyl-3-methoxy-gona-2,5(10)-diene-17-one
Synonyms: Max LMG, 13-ethyl-tren, M-LMG
Originally brought to market as Max-LMG by ALRi, this oddity appears structurally similar to some of the undetectable (at the time) steroids used in the BALCO scandal.
Most steroids are androgens, that is to say they have 19 carbon atoms (17 in the carbon rings of the sterane nucleus, plus two methyl groups attached at C10 and C13). Estranes (more commonly referred to as "19-nors") have no methyl group at C10 (meaning no carbon at the 19th position). Gonanes have no methyl attached at C10 or C13. M-LMG falls into the gonane category as it has no methyl groups, instead it has an ethyl group at C13.
Despite the rather odd-looking double bond structure, upon ingestion the unstable enol ether group will be hydrolysed leaving a ketone at C3, and the 5(10) bond isomerised to the more thermodynamically stable delta-4 position - thus producing 18-methyl-19-norandrostenedione.
Attachment 161
From there it will be converted into the active 18-methyl-19-nortestosterone, and possibly similar estrogenic metabolites. Some of the metabolites may also be progesterone receptor agonists.
User reports would suggest it's a wet bulker carrying a risk of on-cycle gyno, with effects on libido varying from user to user. I'd suggest 4 - 6 weeks cycles at bottle recommended dosages in users who have no predisposition to gyno.
M-Drol
Attachment 162
Nomenclature: 17β-Hydroxy-2α,17α-dimethyl-5α-androstane-3-one or 2a,17a-dimethyl-etiocholan-3-one, 17b-ol or (more accurately) 2a,17a-dimethyl-etioallocholan-3-one, 17b-ol
Synonyms: Superdrol, Methasterone, Methyl Masteron, M-Drol, S-Drol
Originally brought to market by Designer Supplements (then licensed to Anabolic Xtreme), this designer steroid is a 17a-methylated version of the injectable steroid masteron. Since we know 17a-methylation doesn't just increase oral bioavailability, it also changes the effect of the steroid, it may be more useful to consider superdrol as 17a-methyl-DHT with an additional 2-methyl (methyl groups at C1,C2, 17a, and 7a all increase anabolic activity). In fact, superdrol is one of the most potent anabolic steroids ever brought to market. Sadly, it's also one of the most toxic, as evidenced by a number of medical case studies of people hospitalised with cholestatic jaundice and worse. It's for this reason that cycles must be kept short and relatively low dosed. Due to it's structure, it can't aromatise, which means any gyno sides are typically post-cycle. On-cycle lethargy is common, as are shin and back pumps.
Please ignore people who suggest that CEL M-drol is an inferior "b-isomer" version of superdrol, citing the nomenclature as evidence. The fact that they label it etiocholan instead of etioallocholan is a labelling error, not an indication that it contains the wrong compound. People who claim that it's the 5b-reduced isomer fail to understand the dramatic difference that makes to the shape of the steroid (it bends the A-ring away from the plane of the steroid) which dramatically reduces receptor binding affinity (5a-DHT has 173 times stronger binding affinity than 5b-DHT for example). The flatter the better, as far as androgen receptors are concerned. To put it bluntly, if it were the 5b version it would not work (which it does, so it isn't).
Cycles are typically 10 - 30mg for three to four weeks, followed by a SERM PCT protocol.
P-Plex
Attachment 165
Nomenclature: 17a-methyl 5a-androst-2-ene-17b-ol or 17a-methyl-etioallocholan-2-ene-17b-ol
Synonyms: Desoxymethyltestosterone, Madol, Phera-Plex, P-Plex
This long-forgotten steroid, patented in the 1960s but never commercialised legitimately, was rediscovered and distributed to athletes as part of the BALCO scandal. Structurally it is a 17a-methylated version of a naturally occurring pheromone (naturally occurring in elephants, that is), which is where it gets its name. Due to imperfect synthesis techniques (and the difficulty of separation), commercially available phera typically also contains a small amount of the 3-ene isomer. Some of phera's activity may be related to its metabolism in the body into dihydro-dihydroxy-desoxymethyltestosterone (pictured).
Attachment 164
Moderately androgenic while being highly anabolic, this powerful drug delivers rapid size and strength increases and users often report a mild euphoria and heightened libido. Although it cannot aromatise, users may experience some bloating or water retention which may be diet related. Being methylated, liver health must be the main concern when contemplating cycle length and dosage, and I'd suggest 15mg - 45mg for four to six weeks, with the less experienced sticking to the lower end of the scale, followed by an appropriate PCT protocol.
This steroid became a class C controlled drug in the UK in Dec 09, making it illegal to sell (or possess in distribution quantities), and was scheduled in Jan 2010 in the US, making it illegal to sell or possess.
X-Tren
Attachment 166
Nomenclature: 19-Norandrosta-4,9 diene-3,17 dione or estra-4,9 diene-3,17 dione
Despite being commonly known as "tren", this prohormone cannot convert to trenbolone, instead it converts to the similar target hormone of dienolone, which has an anabolic:androgenic ratio of 10:1. Being a dione (and therefore lacking the 17b-OH common to all effective steroids) I'd expect this compound to have little or no affinity for androgen receptor binding in its current configuration. Fortunately the body can convert the ketone to a hydroxyl group via the 17b-HSD enzyme, which will make it much more effective.
This compound should bring strength, lean gains, an increase in vascularity and muscle hardness, and accelerated fat loss.
Support supplements should include an over-the-counter anti-prolactin product such as vitex, B6 or P5P, and one of the common blood pressure supps like celery seed or hawthorne berry. Despite not being 17a-methylated, blood test results typically show a similar degree of hepatic stress to methylated compounds like h-drol or epi. "Shutdown" is usually high, with most users experiencing (temporary) testicular atrophy and loss of libido. Common cycles are 90-120mg for four to six weeks, followed by a SERM PCT protocol.
This compound is illegal in the United States as of Jan 2010, but remains unscheduled in the UK (at the time of writing).
Alpha-One
Attachment 168
Nomenclature: Methyl-1-Etiocholenolol-Epietiocholanolone, or 17a-methyl-1-androstene-3b,17b-diol
Originally marketed by Legal Gear as Methyl-1-Alpha, this is 17a-methylated version of 1-AD, so whereas 1-AD converted to 1-Test, M1AD converts to M1T (aka Methyl 1-Testosterone). While M1T is banned in the US, there is currently no legislation against this "prohormone" to it.
Attachment 174
According to Vida, it's roughly as androgenic as methyl test, but around four times as anabolic (M1T is roughly twice as strong as M1A on both counts, according to the same source). The conversion rate to M1T should be fairly high, plus in its unchanged diol configuration I would expect some receptor affinity. Methyl 1-Test is highly hepatotoxic (more so than most methylated orals), and I don't see why this would be markedly less so, since they are both 17a-methylated (which prevents deactivation through metabolism of the 17b-OH), and the covalent bond structure is the same. This concerns me, as people typically run M1A at several times the dosage of M1T. I guess blood work will tell.
I would not recommend this compound to beginners. Strength and size gains should be rapid and profound, with some of that being due to increased water retention. Side effects may include (but are not limited to) high blood pressure, lethargy, back and shin pumps, loss of sex-drive, and adverse shifts in lipoprotein subfractions. While on paper neither this compound nor its metabolites aromatise, plenty of M1T users have reported on-cycle gyno so it would be prudent to assume a degree of risk with this compound as well.
Cycle lengths should be short and relatively low dosed IMO, two to four weeks at 20 - 40mg (some users will choose to go up to 60mg), followed by an appropriate SERM PCT protocol.
Stano-Drol
Attachment 173
Nomenclature: 3β-hydroxyetioallocholan-17-one; 3β-hydroxy-5α-androstan-17-one
Synonyms: Epiandrosterone, androhard, E-spray
Attachment 175
The Vida data shows that it is almost entirely inactive when injected, only having an extremely mild androgenic effect. This needs to be taken orally (or transdermally) to convert to an active hormone.
This is a prohormone to the naturally occuring testosterone metabolite DHT (dihydrotestosterone). It requires a two-step conversion (via 3b-HSD and 17b-HSD). It will be quite androgenic and not particularly anabolic, so you should get a nice hardening effect, better workout aggression, and a positive effect on libido, but should probably be avoided by those with a propensity to MPB or prostate issues. It isn't a big mass-building drug run solo, but it may be worth stacking with something to offset some of the side-effects of the other compound (for example, if the other drug causes low libido or lethargy).
In December 2009 this compound was added to the list of Class C controlled drugs in the UK under the Misuse of Drugs Act (see part (3)(b)(vi)).
D-Plex
Attachment 178
Nomenclature: 17a-methyl-5a-androstan-17b-ol-3-one oxime, 17a-methyl-5a-androstan-17b-ol-3-hydroxyimine or 17a-methyl-etioallocholan-17b-ol 3-hydroxyimine
Synonyms: d-plex, the one
Originally marketed (aggressively) as "The One" by Applied Nutriceuticals, this is essentially mestanolone (methyl DHT) with a 3-oxime group.
Attachment 177
The Vida data appears promising, demonstrating an anabolic potential nearly four times higher than testosterone, with androgenic qualities only slightly higher than test. This fails to take into account the difference in administration though; this was injected, whereas D-Plex is taken orally.
Taken orally, the oxime group should be fairly efficiently hydrolysed by the stomach acids, leaving plain methyl DHT, and so it can be considered a prohormone to it. Some will survive the acid bath, and the results experienced will be partly from the mestanolone metabolite, and partly from the compound as described by Vida.
The following image gives a visual demonstration of the metabolism of a similar compound:
Attachment 176
I would post the Vida data on methyl DHT but the sources he quotes disagree wildly on the anabolic:androgenic values.
References: 17. Ethers and Nitrogen Derivatives
New designer steroid The One is really just Methyl-DHT
ThermoLife International Forums - View Single Post - Designers
Protodrol
Attachment 179
Nomenclature: 17a-methyl-5a-androst-17b-ol, or 17a-methyl-17b-hydroxy-5a-androstane, or 17a-methyl-etioallocholane-17b-ol, or 17a-methylandrostan-17-ol
Synonyms: Protodrol, desoxymestanolone, desoxymethyldihydrotestosterone, proto-max
Before being launched as "Protodrol" by iForce Nutrition, this compound was mentioned in Vida's book, as well as a couple of medical studies, and like lots of designer steroids was synthesized at one point by Patrick Arnold.
If you thought that the nomenclature looks a lot like methyl DHT, you'd be right. This compound is methyl DHT without the 3-ketone (so it could be described as 3-desoxy mestanolone).
http://i47.tinypic.com/2zdophu.jpg
A 3-ketone usually increases activity, so one could assume from this that methyl DHT would be stronger than its desoxy cousin Protodrol, however the Vida data would suggest otherwise (though it's worth remembering that the different sources Vida quotes often give wildly differing values for the same compounds, so they shouldn't be taken as gospel).
There also exists the possibility that the body is capable of introducing a 3-ketone to protodrol in vivo. This is well-documented with delta4 3-desoxy steroids such as ethylestrenol, but whether it's possible or not with protodrol is unknown.
1. Vida on 3-substitution
2. A more recent study on the effects of 3-substitution
However, the main marketing point of Protodrol wasn't its anabolic or androgenic potential, it was the promise of being the only 17a-methyl to be liver safe.
Despite the relatively small number of symptomatic cases of hepatic injury caused by methylated steroids, liver health is a genuine concern (not least because by the time you are symptomatic, you're already in a bad way). The primary method by which 17a-alkylated steroids induce injury on the liver is by causing a condition called cholestasis, where the liver is unable to excrete toxins into the intestine via the bile ducts. Instead, the liver gets "backed up" and waste products like bilirubin start leaking out into the blood stream (causing the yellow discolouration in the eyes and skin known as jaundice).
3. Info on cholestasis
This condition is typically reversible, but the case studies make for a sobering read. 4.
Click here to view an extract from a study done in 1966 on the hepatotoxicity of various steroids (in rabbits), used in the marketing of Protodrol. 5.
BSP = bromosulfophthalein
6.Quote:
Bromosulfophthalein (BSP) is a relatively nontoxic organic anion used as an in vivo indicator of liver performance. Elimination of BSP via the biliary system following iv injection requires dissociation from albumin in plasma, translocation across the sinusoidal membrane, conjugation with glutathione within the hepatocyte, translocation across the bile canalicular membrane, and excretion in bile.
As you can see, if doses of protodrol failed to impair biliary function in rabbits at such high doses, it bodes well for human use, however it doesn't rule out some degree of hepatic toxicity by other mechanisms.
But what does protodrol do??
Patrick Arnold knocked some up back in '05, and had this to say about it:
7.Quote:
I had some people try it out, one guy in particular who was an old friend in town and was my guinea pig for stuff since back when I first was making 4-AD and its nor analog. Anyway, this guy comes back after six weeks or so and says, “What the hell WAS that stuff?” I asked him what he meant and he said it’s the best stuff he has ever taken. He had clean gains and felt great and his strength was through the roof.
Of course since then there's been a lot more people use this compound, and so for dosage instructions and cycle expectations it would be wise to defer to the user logs and feedback.
References
1. Julius Vida - Androgens and Anabolic Agents, 1969.
2. Structural characteristics of anabolic androgenic steroids contributing to binding to the androgen receptor and to their anabolic and androgenic activities - Applied modifications in the steroidal structure, 2008
3. Br. J. clin. Pharmac. (1983), 15, 3-14
Drug Hepatotoxicity
4. Cholestatic Jaundice and IgA Nephropathy Induced by OTC Muscle Building Agent Superdrol [link]
5. Steroids. 1966 Feb;7(2):157-70.
Effects of various 17-alpha-alkyl substitutions and structural modifications of steroids on sulfobromophthalein (BSP) retention in rabbits.
6. Effect of Cadmium on Bromosulfophthalein Kinetics in the Isolated Perfused Rat Liver System -- Soto et al. 69 (2): 460 -- Toxicological Sciences
7. Over-The-Counter Steroid Products Part II
P-Mag
Attachment 181
Nomenclature: 4-chloro-17a-methyl-androst-4-ene-3b,17b-diol
Synonyms: Promagnon 25, P-Mag, Methyl-clostediol
Another methylated prohormone, this one is often compared to (and mistaken for) a halodrol clone, though there is an important structural difference. P-mag lacks the C1-2 double bond common to boldenone derivatives like h-drol, boldione, dbol and M1,4ADD, having only a C4-5 (delta-4) double bond which makes it a closer structural relative of testosterone and methyl testosterone. The difference becomes apparent when we look at what each one becomes in vivo: where some h-drol is metabolised via 3b-HSD to oral turinabol, p-mag becomes methylated clostebol. A 4-chloro group is common to both drugs, which will make both poor substrates for the aromatase cytochrome P-450 enzyme.
Attachment 180
The target hormone of methyl-clostebol (shown above) appears to be moderately anabolic (about half as strong as methyl test) and not very androgenic, with an overall A:A ratio of somewhere around 3:1 (compared to methyl test). This is a much less impressive ratio than OT, but A:A assays on rats are not definitive (and often conflicting), and compounds with a moderate amount of androgenicity tend to have more positive effects on mood energy and libido than those without.
What's most interesting for me is the choice in bringing out this particular diol prohormone, despite an apparent lack of legislation to prohibit the sale and possession of the target steroid above. I've checked the US Controlled Substances Act [link] and the UK Misuse of Drugs Act [link], and it's not listed on either. This means that theoretically a willing manufacturer would be able to sell methyl clostebol just as legally as p-mag (which is not to say that that is particularly legal in the first place).
Despite being structurally and pharmacologically distinct from h-drol, I suspect p-mag will never quite escape comparisons with it's diene brother. While the effects of h-drol are most apparent in the last few weeks of a six week cycle, p-mag users tend to report more immediate size gains, with a lack of additional weight added in the last couple of weeks. Libido tends to remain more positive, likely due to the more androgenic qualities of the drug.
The aforementioned positive attributes and the possibility of short cycle durations would make this an excellent choice for a first cycle, though as with any methyl it is a good idea to educate yourself about the possibilities of hepatic impairment (watch out for yellowing of the eyes and skin, persistent itchiness especially of the palms and soles of the feet, and discontinue use and see a doctor if either of those occur).
While h-drol has proved popular for bulking, cutting, and recomping, p-mag is generally regarded as best when used for bulking.
Cycles should be somewhere in the region of 50 - 100mg for four to six weeks with an appropriate PCT protocol.
Furaza-A
Attachment 182
Nomenclature: 5a-androstano[2,3-c]furazan-17b-tetrahydropyranol ether
Synonyms: Orastan A, unmethylated furazabol, CTD Winabol, CEL Furaza-A, Axis Labs Furazadrol, Furaguno
Originally marketed by Gaspari as Orastan-A, this is an unmethylated version of the illegal steroid Furazabol (or Androfurazanol), with a THP ether attached to protect the 17b-hydroxyl group.
Attachment 184
Here's the Vida profile for unmethylated furaza [1]. ~100% of the anabolic activity of test prop when injected, with only 30-50% the androgenic activity. Oral administration will be less effective due to first-pass metabolism by the liver.
The THP ether will likely be mostly cleaved by the stomach acids, leaving free unmethylated furaza as shown in the Vida diagram. That which survives with the THP ether intact may be taken up directly into the lymph system from the small intestine, bypassing first-pass liver degradation, since the THP ether increases the lipophilic properties of the drug. One suggestion to increase the amount that survives the initial acid bath etherified would be to dissolve the compound in oil prior to ingestion. This was a popular method a few years ago with 1-test ether gel capsules, though from what I've heard real-world results tended to be disappointing.
One of the more outlandish claims regarding this compound is that it positively impacts cholesterol, however I believe these claims date back to a time when the importance of the lipoprotein subfractions were poorly understood and a decrease in overall cholesterol was considered positive, today we understand that this is likely due to a drop in HDL ("good cholesterol") and is not a positive aspect of a drug's effects.
This compound is to furazabol what prostanozol (or p-stanz) is to winstrol, with unmethylated furaza being generally regarded as the superior of the two. Apparently, furazabol would be stronger if it had a 4-ene, but winny would be weaker with the same double bond [2]. 17α-methyl-4-androstene-2,3-furazan-17β-ol is both more anabolic and more androgenic than furazabol by oral administration according to the following graph:
Attachment 183
The solid thick black line labeled androfurazanol is (illegal) furazabol. The thin dotted line (compound V) is furazabol with a 4-ene.
Compound V is not listed on the US Controlled Substances Act or UK Misuse of Drugs Act, and would therefore be as legal as any of the other grey-market steroids currently sold, if someone were to have it custom synthesized.
DHT-based, with a 2,3 furazan ring system, aromatisation is impossible, so gyno on cycle should not be a concern with Furaza-A. Effects and side-effects will both be somewhat less pronounced than most commonly cycled compounds, yet the original Orastan A had a vocal following who will no doubt be pleased to see it return to the market.
Solo cycles will typically be used to minimise muscle loss while cutting, and it will often be stacked with other compounds for its muscle-hardening effects, lean gains, and relatively low side-effect profile.
I've heard that effects will start to be felt around the 200mg mark, with most users opting for dosages of around 300mg ED, which can start to get quite expensive.
References and further reading:
[1] Androgens and Anabolic Agents, Julius Vida 1969
[2] Investigations on Steroids. V. Pharmacological Studies. (1). Anabolic and Androgenic Activities of 17β-Hydroxy-17α-methyl-5α-androstano[2, 3-c]furazan (Androfurazanol), A New Active Anabolic Steroid by Akira Kasahara,Takeshi Onodera,Michiko Mogi,Yasuo Oshima and Masao Shimizu (click here for the full text, or here to find out how to synthesize them)
P-Stanz
Attachment 185
Nomenclature: [3,2-c]pyrazole-5alpha-etioallocholane-17beta-tetrahydropyranol or 17beta-tetrahydropyranol-5alpha-androstano-[3,2-c]pyrazole
Synonyms: CEL P-Stanz, ALRI Prostanozol, Generic Labz Mega-Zol, unmethylated winstrol.
Prostanozol is an unmethylated version of the popular - but illegal - steroid stanozolol, a.k.a. "winstrol" or "winny". Here's the two structural diagrams side by side:
Attachment 186
[1]
As you can see, although it lacks the 17a-alkylation of winstrol, it has (like the Furaza-A previously discussed) a THP ether to increase bioavailability through uptake by the lymphatic system.
The obvious unique features of these compounds are the furazan and pyrazole rings attached to the A-ring. These are examples of 5-membered heterocycles (another highly amusing example would be Arsole), about which Vida had this to say:
Attachment 187
[2]
While prostanozol is the best legal stanozolol derivative we currently have on the market, just as with furazabol the 4-ene derivative (a steroid I call "testozolol") would be worth considering.
Attachment 188
[2]
Fortunately for us, researchers in the 1960s tested stanozolol and "testozolol" against each other, removing the guesswork from the situation. Displaying 46.5% of the androgenicity and 61.5% of the anabolism of stanozolol by oral administration, although being slightly weaker it should still possess a very positive A:A ratio, and according to the researchers, some estrogenic activity. [3]
Much like Furaza-A, Prostanozol is a mild compound likely to be expensive to run at effective doses, and will be best used either solo to retain muscle mass while cutting, or in conjunction with another compound to add hardening effects and lean gains without adding too much to the overall toxicity and side-effects of a cycle.
Prostanozol was added to Schedule 2 of the UK Misuse of Drugs Act 1971 (effective 23rd December 2009), making it illegal to sell, and illegal to possess in distribution quantities in the UK. It remains unscheduled (at the time of writing) in the US. [4]
References:
[1] Journal of Steroid Biochemistry & Molecular Biology 101 (2006) 161–178
[2] Julius Vida, Androgens and Anabolic Agents
[3] Influence of molecular unsaturation on hormonal activity pattern of certain heterocyclic steroids
[4] The Misuse of Drugs Act 1971 (Amendment) Order 2009
Boladrol
Attachment 189
Nomenclature:
7a,17a-dimethyl-androsten-3b,17b-diol
Anabolic/Androgenic Ratio:
Unknown. The anabolic/androgenic ratio for the target hormone of Bolasterone is around 1300:300 vs. methyl test by oral administration. [1]
Synonyms:
7a,17a-dimethyl-androst-4-en-3b,17b-diol, Boladrol, Bolasterone diol, Dimethylandrostenediol.
History:
This is a brand new prohormone from PHF/IBE, never seen before on the prohormone or pharmaceutical market, that converts in vivo to the steroid Bolasterone. Bolasterone was invented in 1959 [2], and in 1962 was described as "the most potent oral anabolic agent which had yet been examined" [3].
Structure and Function:
Boladrol is a "diol" prohormone, and should convert well to the active hormone via the same mechanism as all 3b,17b-diols: the enzyme 3-β-hydroxysteroid dehydrogenase, or 3b-HSD.
Structurally, Boladrol is a testosterone derivative, having the C3-C4 double bond common to this class of hormone. It resembles methyl testosterone in that it has a 17a-methyl group, though differs from it in that it has an additional methyl group at position 7a, and a hydroxyl at position 3b, whereas methyl test has a 3-ketone function. The addition of the methyl group at 7a greatly increases both the androgen receptor affinity and the anabolic properties of the compound [4].
Structurally it would appear likely to aromatise to a potent dimethylated estrogen, though the 7a-methyl may provide steric hindrance to the reaction. In fact there's evidence that some 7a-alkylated testosterone derivatives have aromatase inhibiting properties, with smaller 7a substitutions making stronger inhibitors than bulkier substitutions. [5]
This 7a-methyl group will also prevent the steroid from being 5a-reduced, but does not prevent it from being 5b-reduced, so all metabolites lacking the delta-4 double bond will be (inactive) 5b-reduced metabolites, as you can see from the image below. [6]
Attachment 190
The metabolites 2, 4, and 5 above are described further here [7]:
Attachment 191
Effects:
Effects should be similar to the oral anabolic steroid Bolasterone. It's a strongly anabolic, moderately androgenic compound which should elicit significant strength gains and increased accumulation of muscle mass at an appropriate dosage.
Since it's a powerful compound, and aromatisation a likelihood, weight gain is likely to be quick with the user's gains resulting from a mix of acquired muscle mass and a mild increase in water retention on cycle. A SERM PCT protocol should be followed upon cessation.
Side Effects:
The androgenic potential of the compound may have been exaggerated, at least at appropriate dosages, since the anabolic:androgenic ratio of about 4:1 vs. methyl test is not particularly low (especially since test has an A:A of 1:1). Also, low-dosed human testing reported no androgenic side-effects in any users [8].
Side-effects may include (but are not limited to): loss of or heightened libido, elevated liver enzymes and potential temporary liver function impairment, HPTA disruption, adverse shifts in lipoprotein subfractions (lowered HDL, increased LDL cholesterol), acne, hair growth or loss, and an increase in blood pressure. This product should not be used by women or teens.
Recommended Dosages and Cycle Durations:
The clinical evaluation of Bolasterone in the 1960s found it to be effective at promoting weight gain at doses of just 1-2mg. They also found it to be around twice as potent as dianabol by nitrogen retention studies [8]. Bodybuilders typically use dosages several times higher than those administered clinically.
As with any new compound, sensible users will keep dosages low and cycle-lengths short, until those with less caution have established some guidelines of how not to do it (by finding the dosages at which unacceptable side effects are encountered). Early Boladrol adopters have been dosing between 4 and 8mg per day for two to four weeks, and reporting great results.
References:
[1] Structure and effects of anabolic steroids. Pharmacol Ther B 1975;1:233–75.
[2] J Am Chem Soc 1959;81:4069-74.
[3] International Congress on Hormonal Steroids, Milan, Italy, 1962, Excerpta Med., Internat. Congr. Series No. 51.
[4] Steroids. 2009 Feb;74(2):172-97.
[5] Steroids Volume 40, Issue 6, December 1982, Pages 603-614
[6] Clinical Chemistry 42:7 1001-1020 (1996)
[7] J Steroid Biochem Mol Biol. 2009 May;115(1-2):44-61.
[8] Clin Pharmacol Ther. 1963 Nov-Dec;4:734-9.
Delta-2 (2-Androstenone)
Attachment 192
Nomenclature:
5a-androst-2-ene-17-one or 2-androsten-17-one
Anabolic/Androgenic Ratio:
Unknown. The active version of this prohormone, 2-androstenol, was found to have no activity by oral administration according to the researchers at Searle, [1] though this may be because 2-androstenol is not water soluble and so cannot be absorbed by the small intestine - unlike 2-androstenone. [2]
Suffice to say that it is relatively weakly active (meaning that it needs to be dosed fairly high), much like many other non-17a-alkylated prohormones (such as 11-oxo, 4-AD, and boldione).
Synonyms:
Delta-2, 2-androstenone
History:
While 2-androstenol was previously released as one of the two compounds in Anabolc Xtreme's 3-AD (the other being androsterone), 2-androstenone was new to the market in 2011.
In fact, two unaffiliated companies brought out the compound roughly simultaneously: AndrogenetX in the US and Fusion Supplements in the UK.
Structure and Function:
This non-methylated compound possesses the Δ2 double bond as found in the designer steroid desoxymethyltestosterone (a.k.a madol, pheraplex), therefore it lacks the 3-keto function common to most anabolic steroids.
The easiest way to think about this compound is as a prohormone to unmethylated pheraplex (desoxymethyltestosterone). Like DHEA or 4-androstenedione it has a 17-keto function, which will be reduced by interaction with the 17bHSD enzyme in vivo to the active hormone 2-androstenol (unmethylated phera). This 17b-hydroxylated metabolite will be the one responsible for the anabolic and androgenic effects seen with this drug.
Effects:
Like all anabolic steroids, the user can expect a marked increase in protein synthesis leading to a much faster rate of muscle accumulation, along with a significant boost in strength. Aromatisation should be impossible (due to the lack of a 3-keto and 4-ene), though as with all non-aromatising androgens that does not mean that estrogen-related side-effects are impossible (just much less likely).
Side Effects:
There's some supposition that pheraplex is an inhibitor of 11b-hydroxylase, which would account for the apparent water retention ("bloat") and high blood pressure some users experienced, despite the fact that phera doesn't aromatise to estrogen. Inhibition of 11b-hydroxylase can lead to increased renin secretion which results in higher levels of aldosterone, a mineralocorticoid that causes high blood pressure and water retention through sodium retention and the excretion of potassium. [3]
One study on bodybuilders found far higher levels of aldosterone in the steroid-taking group than in the non-steroid taking group - and these changes remained far past the end of their cycles. [4]
Whether or not this is the case for 2-androstenone - or phera for that matter - remains to be proven, but it is food for thought, particularly as a previous study pointed the finger at aldosterone as a cause of left ventricular hypertrophy, and suggested that it's heart remodelling effects may be unrelated to it's blood-pressure increasing effects. [5]
On balance though, this is likely to be one of the safer compounds on the market, due to the lack of liver-damaging 17a-methylation, lack of aromatisation, and possible "feel good" qualities if it shares that quality with it's big brother pheraplex.
The side effects common to all oral steroids, as discussed in the other writeups in this series, will also apply here.
Recommended Dosages and Cycle Durations:
There's a lack of solid feedback from users at the point of writing, though I would suggest doses in the range of 300mg upwards, with most users seeing best results around 600mg/day for a period of four to six weeks, followed by an appropriate PCT protocol and period of discontinuation.
References:
[1] J. Med. Chem., 1966, 9 (5), pp 693–697
[2] New prohormone: Delta-2
[3] Cardiovascular Toxicity of Anabolic Steroids, Annual Review of Pharmacology and Toxicology Vol. 33: 497-520
[4] Aldosterone Concentrations in the Blood Plasma and in the Urine Samples as the Biological Marker of Anabolic Adrogenic Steroids (AAS) Abuse, Recent advances in doping analysis (12). Sport und Buch Strauß, Köln (2004) 395-401
[5] New perspectives on the role of aldosterone excess in cardiovascular disease. Clin Exp Pharmacol Physiol. 2001 Oct;28(10):783-91.
Epistane/Havoc
Attachment 194
Nomenclature:
2a,3a-epithio-17a-methyl-5a-androstan-17b-ol or 2a,3a-epithio-17a-methyl-etioallocholan-17b-ol
Anabolic/Androgenic Ratio:
1100:91 vs. methyl test by oral administration [1]
Synonyms:
Epistane, Havoc, Epi, E-Stane, Epi-Strong, Methylepithiostanol
Etymology:
Methylepithiostanol: Methyl indicates the 17a-methyl group, epi means above, indicating the bridge, thio indicating sulphur, stan is short for the androstane skeleton, and ol points out the hydroxyl at 17b.
History:
One of a number of steroidal compounds researched in the 60s by Searle Laboratories, while it was never used clinically in the West, the unmethylated analog epitiostanol has been used to treat breast cancer and gynecomastia in Japan. [2][3]
The two first "prohormone" products containing this compound, IBE's Epistane and RPN's Havoc, are still the two best-selling "epi" products on the market.
Structure and Function:
Resembling methyl DHT, but with a sulphur atom spanning C2 and C3, methylepitiostanol is an orally active compound that lacks the 3-ketone common to most anabolic steroids. Some of it's activity will be due to metabolism in vivo to other active compounds - including desoxymethyltestosterone (pheraplex). [4]
It will undergo dethionylation (loss of the sulphur atom) both in vivo or via pyrolysis (administration of high temperatures) to produce phera, as illustrated in this diagram. [5]
Attachment 193
Effects:
Greatly increased protein synthesis and accrual of lean muscle mass with attendant strength gains. Some fat loss may be experienced, though this is dependent on diet and training.
Side Effects:
Side-effects may include (but are not limited to): loss of or heightened libido, elevated liver enzymes and potential temporary liver function impairment, HPTA disruption, adverse shifts in lipoprotein subfractions (lowered HDL, increased LDL cholesterol), acne, hair growth or loss, and an increase in blood pressure. This product should not be used by women or teens.
Gains are very lean and dry with many users complaining of sore joints (so a joint supp like Joint Force would be recommended to those experiencing pain or discomfort).
Recommended Dosages and Cycle Durations:
Cycles are typically 30 - 40mg daily for four to six weeks, followed by a SERM PCT protocol to avoid "rebound gyno".
References:
[1] Anabolic agents. 2,3-Epithioandrostane derivatives. J. Med. Chem., 1966, 9 (5), pp 693–697
[2] Gan To Kagaku Ryoho. 1988 Jul;15(7):2163-7.
[3] Jpn. J. Clin. Oncol. (1973) 3 (2): 99-104.
[4] Xenobiotica. 1991 Jul;21(7):865-72.
[5] Drug Test Anal. 2009 Nov;1(11-12):518-25.
M1T
Attachment 195
Nomenclature:
17a-methyl-1-testosterone, or 17a-methyl-17b-hydroxy-1-androsten-3-one, or 17a-methyl-5a-androst-1-ene-3-one-17b-ol
Anabolic/Androgenic Ratio:
910-1600:100-220 vs. methyl test by oral administration. [1][2]
Synonyms:
Methyl-1-testosterone, 17aa-M1T, M1T, Methyl Dread, M-One-T, 17a-methyl-dihydroboldenone
History:
It was originally synthesized as early as 1962 at Searle Laboratories though, like most compounds researched in the 1960s, never made it as far as human testing. Although it was extremely anabolic, it also possessed fairly strong androgenic qualities and was consigned to the annals of history, until it was unearthed decades later to take the bodybuilding supplement industry by storm.
M1T was the culmination of an arms race in the industry during the late 90s and early 2000s that started when Patrick Arnold released the prohormone to testosterone 4-androstenedione. He then followed it up with the hugely popular 1-androstenediol, a 1-testosterone precursor. Other firms took this one step further by producing the already-active 1-testosterone, and finally Legal Gear (now LG Sciences) upped the ante by bringing to market Methyl 1-Testosterone (M1T), which unlike the previous compounds was an entirely synthetic (non-naturally occurring) fully active oral steroid. [3]
The popularity of this and other synthetic hormones (along with a couple of sports doping scandals) attracted a lot of unwanted attention to the industry, resulting in the Anabolic Steroid Control Act of 2004 which saw M1T, 1-AD, 4-AD, and every prohormone and steroid the US govt. could think of added to Schedule III of the Controlled Substances Act, making them illegal to sell or possess, [4] though no legislative action has been taken against it in the UK at the time of writing.
Structure and Function:
This is a 17a-methylated compound, making it highly orally available. It lacks the delta-4 double bond of testosterone, having a 1,2 double bond instead. This means that it will not aromatise, and it will not 5a-reduce in androgen-sensitive tissues like testosterone can (since it's 5a-reduced already). Metabolism is limited, to a large extent, to reduction of the double bond and hydroxylation of the 3-ketone. [5]
Attachment 196
Fig 1. Metabolism of 1-androstenes [6] (image simplified for illustrative purposes).
Effects:
Users can expect significant and rapid weight gain accompanied by extreme gains in strength. This is not a compound to be underestimated and would be well-suited to those looking for immediate results. Some of the weight gained will be in the form of fluid retention that will be lost upon cessation, though long-lasting physique improvements can be made by taking full advantage of the short highly anabolic window of the cycle.
Side Effects:
Many have assumed that M1T aromatises, however that is structurally impossible. What is possible - and much more likely in my opinion - is that it is an inhibitor of 11b-hydroxylase, which would account for both the apparent water retention ("bloat") and high blood pressure some users experience.
Inhibition of 11b-hydroxylase can lead to increased renin secretion which results in higher levels of aldosterone, a mineralocorticoid that causes high blood pressure and water retention through sodium retention and the excretion of potassium. [7]
One study on bodybuilders found far higher levels of aldosterone in the steroid-taking group than in the non-steroid taking group - and these changes remained far past the end of their cycles. [8]
This may or may not be the case for M1T (and many other steroids), but it is food for thought, particularly as a previous study pointed the finger at aldosterone as a cause of left ventricular hypertrophy, and suggested that it's heart remodelling effects may be unrelated to it's blood-pressure increasing effects. [9]
Liver toxicity is also a concern with this compound. While there are many 17a-methylated compounds on the market, they are not all equally hepatotoxic at like-for-like dosages. Protodrol for example is likely to impart minimal hepatic impact at doses of 100mg for six weeks, while 20mg of M1T for a couple of weeks will significantly adversely affect liver function markers. Abuse of this drug with high doses for long periods of time can result in intrahepatic cholestasis (jaundice), and for this reason cycles should be kept short, low-dosed, and alcohol-free.
Recommended Dosages and Cycle Durations:
Most trainees should see dramatic results at 10mg/day for two to three weeks, the cautious may do well on 5mg, while the more reckless will use higher doses and durations. Although cycles are short, it's a strong suppressive compound, so a full SERM PCT protocol is advised.
References:
[1] Acta Endocrinol December 1, 1966 53 635-643 [link]
[2] J. Med. Chem., 1965, 8 (1), pp 48–52 [link]
[3] The History Of Pro-Hormones on Super Human Radio
[4] Senate Bill 2195
[5] Recent Advances in Doping Analysis (14), Sport und Buch Strauss, Cologne, Germany, 2006, pp. 249–258.
[6] J Steroid Biochem Mol Biol. 2009 May;115(1-2):44-61.
[7] Cardiovascular Toxicity of Anabolic Steroids, Annual Review of Pharmacology and Toxicology Vol. 33: 497-520
[8] Recent advances in doping analysis (12). Sport und Buch Strauß, Köln (2004) 395-401
[9] Clin Exp Pharmacol Physiol. 2001 Oct;28(10):783-91.
M4ohn
Attachment 197
Nomenclature:
4-hydroxy-17a-methyl-19-nortestosterone or 4-hydroxy-17a-methyl-17b-hydroxyestr-4-en-3-one or 17a-methyl-3-oxo-19-norandrostene-4,17-diol
Anabolic/Androgenic Ratio:
1304:281 vs. methyl testosterone by oral administration, and 1304:1024 vs. methylnortestosterone by oral administration. [1]
Synonyms:
M4OHN, methyl hydroxy nandrolone, MOHN, oxavar
History:
This compound is first described in the literature in 1964, when researchers from Milan, Italy, explored the effects of adding a hydroxyl group at C-4 to a variety of steroids. [2]
It was launched on the prohormone market in 2004 as a bulk powder by Designer Supplements and 1fast400. The first capped product was Oxavar by Gaspari Nutrition.
It was shortlived, however, since the Anabolic Steroid Control Act of 2004 [3] saw it added to Schedule III of the Controlled Substances Act, making M4OHN illegal to sell or possess in the USA. It resurfaced in the UK in late 2010; no legislative action has been taken against it in the UK at the time of writing.
Structure and Function:
This is a oral nandrolone-derived steroid. It differs from nandrolone in that it has a 17a-methyl group to improve oral bioavailability, and a 4-hydroxyl group that increases the dissociation of anabolic and androgenic effects. It is essentially a 19-nor version of the steroid oxymesterone.
G. Sala, in his paper on the biological properties of 4-hydroxy-3-keto-Δ4-steroids [2], observed that "4-hydroxy-17a-methyl-19-nortestosterone presents a strong increase of the myotrophic and of the androgenic effect, with a moderate increment of the therapeutic index, as compared with 17a-methyl-19-nortestosterone".
This increase in effect was only seen with oral administration, not with subcutaneous injection of the compound, so he goes on to say that he believes this is due to the hydroxylation at C4 increasing "intestinal absorption of 17a-methyltestosterone derivatives", in addition to "favoring dissociation between myotrophic and androgenic activity".
The 4-hydroxyl group also abolished the progestational effects of all of the testosterone and nortestosterone derivatives studied. The results of his observations of the compound are summarized below:
Attachment 198
The addition of the 4-hydroxyl function is likely to hinder (though not prevent) the reduction of the C-4,5 double bond. This is particularly true of 17a-methylated steroids such as this one. [4]
Whereas testosterone derivatives typically 5a-reduce to stronger androgens, 19-nortestosterone derivatives typically 5a-reduce to weaker androgens. This goes some way to explaining why M4OHT (methyl hydroxy testosterone) is more anabolic and less androgenic than methyl test, while M4OHN (methyl hydroxy nandrolone) is more anabolic and much more androgenic than methyl nandrolone.
Effects:
While the anabolic:androgenic profile would suggest that this was a strong mass-builder, user feedback would suggest it is instead an effective cutter and best used by those looking to shed excess fat.
Side Effects:
One of the issues surrounding nandrolone derivatives, particularly 17a-methylated nandrolone derivatives, is their potential for progestational activity. Fortunately this compound is an exception to the rule, having no progestational effects. Any nipple sensitivity on-cycle will therefore be estrogen related and should be dealt with by a SERM or aromatase inhibitor.
The standard list of steroidal side-effects listed in the other profiles will also apply to this compound.
Recommended Dosages and Cycle Durations:
Due to it's strong profile this compound was originally released in 2mg caps, with other manufacturers dosing them similarly at 2-4mg. Users often ran it much higher, with 12mg being common though some reported the best effects at 40mg or even higher.
The clone currently available on the UK market is dosed at 10mg per cap, which will make it much easier and more cost-effective to experiment with higher dosing. Since it's a methylated compound cycles are generally 6 weeks or less to minimise the risk of hepatic injury.
References
[1] Vida J.: Androgens and Anabolic Agents. Academic Press, New York (1969) p. 280.
[2] Hormonal Steroids Vol 1, p.67. Academic Press, New York, 1964.
[3] Senate Bill 2195
[4] J Steroid Biochem Mol Biol. 2009 May;115(1-2):44-61.
Methyl Stenbolone
Attachment 199
Nomenclature:
2,17α-dimethyl-5α-androsta-1-en-17β-ol-3-one, or 2,17a-Dimethyl-17b-hydroxy-5a-androst-1-en-3-one
Anabolic/Androgenic Ratio:
660:90-170 vs. methyltestosterone by oral administration. [1]
Synonyms:
Methyl stenbolone, methyl sten, 17a-methyl-stenbolone, m-sten, ultradrol
History:
In 1966, researchers at Searle Laboratories set about methodically testing the myotrophic (anabolic) and androgenic effects of a series of A-ring modified androstane derivatives [2]. The compounds they explored reads like a who's who of designer steroids.
Methyl-1-testosterone (M1T), desoxymethyltestosterone (phera), 17a-methyl-1-androstenediol (Alpha One), and a variety of other 1- and 2-dehydro compounds were explored for activity.
The researchers proudly announced that "Even the least active compound in Table 6 possessed a higher relative myotrophic potency than previously has been obtained with several clinically interesting compounds which have been studied under identical conditions, i.e. oxymetholone, oxandrolone, stanozolol, and methandrostenolone." (anadrol, anavar, winstrol, and dianabol).
Attachment 200
[2]
Key:
IIe = methyltestosterone
IIa = methyl-1-testosterone
IVd = methyl stenbolone
IIf = alpha one (17a-methyl-1-androstenediol)
IIIa = phera (desoxymethyltestosterone)
As you can see from the table above, methyl sten has somewhere between 2/3 and 3/4 the anabolic activity of methyl-1-testosterone, and a similar A:A ratio (by oral administration to castrated rats).
It can also be found in an earlier paper by two of the same authors [3], however at the time it was only studied for activity by intramuscular injection, so the figures it quotes are irrelevant for our purposes. It does, however, give a recipe for producing the compound from superdrol.
Attachment 201
Methylsten™ is listed as one of the ingredients in a proprietary blend in a now-discontinued product called Mass Tabs by IDS, though testing has shown that this product (at least the later, bottled batches) in fact contained superdrol [4][5].
Structure and Function:
Structurally resembling the bastard child of M1T and superdrol, methyl sten is a DHT-derivative that is dimethylated at C-2 and C-17 (like superdrol) and has a 1-ene (like methyl-1-test).
It's important to note that while methyl stenbolone is dimethylated at C-2 and C-17 like superdrol, the spatial configuration is different due to the presence of a delta-1 double bond (the C-2 methyl group is therefore planar). This means that methyl sten is a 2,17a-dimethyl rather than a 2a,17a-dimethyl compound.
A more recent (2009) paper on the effects of structural modifications to steroids concluded that the addition of a 2-methyl function to a 1-ene steroid had little effect on the relative potency of the compound [6].
Attachment 202
[6]
You'll note however that this is view is taken virtually word for word from the 1961 study that only examined the activity of the compounds by IM injection and is therefore questionable when discussing their oral activity.
http://i51.tinypic.com/2qak3h5.jpg
[3]
Metabolism:
Since it's DHT-derived, aromatisation is impossible. 5a-reduction is also impossible, since it's already 5a-reduced. The 17a-methyl group greatly increases the bioavailability of the compound by oral administration.
The combination of delta 1-dehydrogenation and 2-methylation is likely to make the A-ring very resistant to metabolism. 3z-,16z-, and 18-hydroxylated metabolites are likely to be the only ones detectable after administration, other than the unchanged compound [7][8].
Effects:
It is a strong oral steroid in the vein of pheraplex, superdrol, and M1T. It should be an excellent bulking compound at an appropriate dosage.
Side Effects:
It is inevitable that the compound will display some degree of hepatotoxicity. This is discussed in some detail on the manufacturer's blog, which I would recommend reading [9].
The standard list of steroidal side-effects listed in the other profiles will also apply to this compound.
Recommended Dosages and Cycle Durations:
These will be formed by the weight of public opinion after enough logs have been recorded. The only confirmed product on the market to contain this compound comes in 4mg caps and recommends dosing at two caps per day, and not to exceed three caps per day. It is likely in my opinion that the "standard dosing" will end up significantly higher (20mg+).
Given that the level of liver toxicity is at this stage unknown, cycles should be kept to four weeks or less, as is usual with a strong methyl such as superdrol or M1T.
References
[1] Vida J.: Androgens and Anabolic Agents. Academic Press, New York (1969) p. 212.
[2] Acta Endocrinol 1966 53 627-634 & 635-643
[3] J. Org. Chem., 1962, 27 (1), pp 248–253
[4] test results IDS mass tabs - ThermoLife International Forums
[5] Affidavit for bodybuilding.com raid: image 1, image 2, image 3
[6] Steroids 74 (2009) 172–197
[7] J. Steroid Biochem. Mol. Biol. 115 (2009) 44-61.
[8] J. Steroid Biochem. Mol. Biol. 101 (2006) 161–178.
[9] Antaeus Labs: A few words on the hepatotoxicity of 17a-methylated androgens/anabolics
Images simplified for illustrative purposes
With thanks to j3ff_beck.
Trenavar
Attachment 203
Nomenclature:
Estra-4,9,11-triene-3,17-dione
Synonyms:
Trenavar, Trendione
History:
This is a brand new prohormone from PHF/IBE, never seen before on the prohormone or pharmaceutical market.
Function:
This is a prohormone to the veterinary drug and black-market bodybuilding steroid trenbolone. Unlike previous "tren" prohormones, this one actually converts in the body to trenbolone. Previous "tren" PHs converted to the structurally similar - but markedly weaker - steroid dienolone.
Structure:
This prohormone has the same three conjugated double bonds as trenbolone, and differs from it only in that this hormone has a 17-ketone, where trenbolone has a 17b-hydroxy function. In the body this ketone will be readily hydrolysed by 17b-hydroxysteroid dehydrogenase type 5 (17b-HSD5) into the active form, trenbolone.
Effects:
Conversion to trenbolone should be high, so effects should be identical to the injectable form - with the exception of the famed "tren cough". Whatever the explanation for "tren cough" (and many have been suggested), since it's a reaction to the sudden parenteral introduction of some compound directly into the body, it's highly unlikely that any orally administered compound will have the same effect.
Trenbolone is one of the strongest injectable steroids on the market, so effects experienced from Trenavar can be expected to be largely the same - huge strength and size increases, accelerated fat loss, and enhanced vascularity.
Side Effects:
Blood pressure is likely to be dose-dependently elevated to a significant degree, cholesterol levels and liver function markers are likely to be adversely affected, though to what extent remains to be seen. Commonly reported trenbolone sides include night-sweats, mood swings, androgenic hair loss and/or growth, temporary loss of libido, as well as the suppression of endogenous testosterone production, and it would be sensible to assume that these may also result from use of Trenavar.
Metabolism and Bioavailability:
Warning: if you're not interested in advanced steroid metabolism discussion, skip over this section. If you want solid info on how and why an oral tren PH should work, read on.
The anabolic effects of trenbolone are due in part to the enhanced androgen receptor binding that the conjugated double bond system causes [1], and also because trenbolone is an antagonist of the glucocorticoid receptor [2]. The double bonds extending up the backbone of the steroid flattens the steroid considerably, which makes it an excellent fit for the androgen receptor. It also makes the molecule much more flexible, and therefore less receptor-specific [3]. Trenbolone is incapable of being affected by 5a-reductase, 5b-reductase, or aromatase. But will it work orally?
The first place to turn to for information on steroids is the seminal 1969 work Androgens and Anabolic Agents by Julius Vida. Unfortunately this compound isn't among the 666 compounds discussed there, and there's a shortage of information on trenbolone by oral adminstration. I was fortunate enough to find a study which compared the anabolic effects of oral and subcutaneous application of trenbolone in rats [4], and the results were frankly startling. They found that to have a comparable anabolic effect, trenbolone needed to be administered orally at 100 times the dosage as when administered by subcutaneous injection (see graph). Sounds pretty bad for a tren PH then, right? Well, the good news is we're not rats.
Trenbolone is metabolised differently in different species - in rats, around 40% is excreted as a dione form, as well as several metabolites hydroxylated in various positions [5], but in man only one metabolite has been identified - the 17a-epimer [6].
Attachment 204
The ratio of excreted trenbolone (17b-trenbolone) to epitrenbolone (17a-trenbolone) is estimated at 1:5 in a 24hr period [7].
What this means is that although Trenavar is a prohormone to trenbolone, it doesn't appear to be a significant metabolite in humans. The equilibrium of the reaction between 17-one and 17b-ol appears to be weighted heavily - in fact pretty much exclusively - in favour of the 17b-ol, so Trenavar should convert readily to the active form trenbolone. Once converted to trenbolone, it will be open to the same metabolism mechanisms as injectable tren - conversion via sulfatase to epitrenbolone and excretion as glucoronides.
Of course, this is largely conjecture, since neither trenbolone nor a precursor to it has ever been on the supplement market before... or has it?
A few years ago ALRI released an encapsulated product called "Methoxy TRN", advertised as containing "17b-methoxytrienbolone". This was quickly pulled from the shelves soon after its release, leaving only a few highly-collectable bottles and a reputation for tremendous strength and size gains and roadmap vascularity. This supplement was tested in 2008, and the researchers discovered the tell-tale mass spectra of trenbolone (and no sign of the advertised methoxy group) [8].
Detection Limits:
An anti-doping study from 1996 found that orally administered trenbolone was detectable by mass spectrometry for two to four days after a single administration, unlike injectable trenbolone, which is detectable for much longer [9]. The detection of trenbolone after administration of Trenavar is likely to follow similar lines, though detection methods may have improved since then. Athletes subjected to doping tests should of course avoid this and all other prohibited performance-enhancing products altogether.
Dosages and Cycle Durations:
Empirical evidence is the only way to determine this; once the product has been used by enough people we'll have a better idea of how much, and for how long, Trenavar is best used.
References
[1] Steroids 74 (2009) 172–197
[2] Acta Endocrinologica, Vol 110, 1 Suppla, S129-S130
[3] J Steroid Biochem 1979;13:45–59.
[4] Toxicol Sci. 2002;70:202–211.
[5] Xenobiotica. 1981 Jul;11(7):489-500.
[6] Biol. Mass Spectrom. 20 (1991) 459–466.
[7] Recent advances in doping analysis (2). (1995) 269-274.
[8] Anal Chim Acta. 2009 Apr 1;637(1-2):92-100.
[9] Recent advances in doping analysis (3). (1996) 83-94.
Mentabolan
Attachment 205
Nomenclature:
7a-methyl-estra-4-en-3,17-dione
Anabolic/Androgenic Ratio:
960 : 165 - 510 vs testosterone by oral administration [1]
Synonyms:
7a-methyl-19-norandrostenedione, Mentabolan, MENT dione, Trestione.
History:
This is a brand new prohormone from PHF/IBE, never seen before on the prohormone or pharmaceutical market. It was synthesized and tested for anabolic and androgenic activity in rats in 1963 [1].
Function:
This is a prohormone to the black-market bodybuilding steroid and experimental contraceptive Trestolone, aka MENT. It's been described on some internet forums as "MENT dione", however since MENT is short for 7a-Methyl 19-Nor-Testosterone, this compound could more accurately be described as 7a-Methyl-19-Nor-Androstenedione, and given an acronym of it's own like MENAD or MENORAD.
Structure:
This prohormone is a "19-nor", or nandrolone derivative, and differs from nandrolone in that this hormone has a 17-ketone, where nandrolone has a 17b-hydroxy function, and also has the addition of a 7a-methyl group. In the same way as "Boladrol" is a 7a-methylated dione version of methyl testosterone, this compound is a 7a-methylated dione version of nandrolone.
Please don't confuse this compound (or the target steroid) with the widely-feared mibolerone, a.k.a. "cheque drops", which is a 17a-methylated version of trestolone (or dimethylated nandrolone). While MENT has the 7a-methyl/19-nor combination that produces a far stronger steroid than either configuration does alone, it lacks the 17a-methyl group that tends to dramatically increase liver toxicity.
Effects:
Effects should be similar to the injectable trestolone acetate. It's a strongly anabolic, moderately androgenic compound which should elicit significant strength gains and increased accumulation of muscle mass at an appropriate dosage. Users may also experience mood changes, such as an increase in confidence and subjective well being, and/or an increase in workout aggression.
Side Effects:
Side-effects may include those common to anabolic androgenic steroids, including but not limited to: blood pressure increases, HPTA disruption, adverse shifts in lipoprotein subfractions (increased LDL, lowered HDL cholesterol), acne, hair growth or loss. This product should not be used by women or teens. There's evidence that MENT aromatizes to some degree [2], so the gyno-prone may wish to either avoid this compound or co-administer an aromatase inhibitor (AI) or selective estrogen receptor modulator (SERM).
One side-effect that many might fear from this compound is the loss of libido and/or erectile dysfunction often seen with 19-nor derivatives (known colloquially as "deca-dick"). On the contrary, tests conducted with the target hormone trestolone (MENT) have found that it had a positive mood, libido, and erection-stimulating effect similar to that of testosterone [3], though this may not necessarily hold true with the supraphysiological doses used by bodybuilders.
Metabolism and Bioavailability:
As mentioned, this is a "dione" prohormone. In the body the ketone at C17 will be hydrolysed by 17b-hydroxysteroid dehydrogenase type 1 (17b-HSD1) into the active compound trestolone (MENT). Trestolone itself has been shown to be roughly 6 times as anabolic as methyl test by oral administration, and around 2.5 times as androgenic [4].
Unlike steroids like testosterone and DHT, trestolone shows no affinity for SHBG [5], so all of the converted compound in circulation should be bioavailable. For the same reason, it's likely to have a short terminal half-life so frequent dosing is suggested.
As most will know, testosterone and similar delta-4 steroids are typically converted to stronger compounds like DHT and DHT derivatives by the enzyme 5-alpha reductase (5AR). 19-nor compounds are an exception to this rule, with 5a-reduced nandrolone (or 19-nor DHT) being a far less potent androgen than nandrolone itself [6]. The 7a-methylation of trestolone (and by extension Mentabolan) hinders the reduction of this double bond, so delta 5(10) isomers are a major excreted metabolite [7]. This means that the 7a-methyl group not only makes the compound stronger by increasing androgen receptor affinity [8], but also reduces the ability of the body's enzymes to break it down into weaker metabolites.
MENT is a strong compound for several reasons (including as previously discussed steric hindrance to 5a-reduction, and an inability to bind with SHBG), but the primary reason for its strength is the increased androgen receptor affinity caused by the conformational changes of the 7a-methyl group [8][9]. The same will be true of the prohormone to MENT; Mentabolan.
References:
[1] Steroids 1, 299 (1963)
[2] J Steroid Biochem Mol Biol. 1994 Feb;48(2-3):297-304.
[3] J Clin Endocrinol Metab. 1999 Oct;84(10):3556-62.
[4] Acta Endocrinologica, Vol 43, Issue 3, 399-411
[5] J Androl. 1997 Jul-Aug;18(4):352-8.
[6] The Journal of Steroid Biochemistry and Molecular Biology Volume 53, Issues 1-6, 1995, 253-257
[7] Recent advances in doping analysis (12). Sport und Buch Strauß, Köln (2004) 261-268
[8] Steroids. 2009 Feb;74(2):172-97.
[9] The Journal of Steroid Biochemistry and Molecular Biology Volume 71, Issues 5-6, 1999, 213-222
Methyldiazirinol
Structural Image:
http://www.totalflexblog.com/wp-cont...-structure.jpg
Nomenclature:
3,3-azo-17a-methyl-5a-androstan-17b-ol or
3,3-azo-17α-methyl-5α-androstan-17β-ol
Read the full profile here.
Dimethandrostenol
Structural Image:
http://www.totalflexblog.com/wp-cont...ndrostenol.jpg
Nomenclature:
2,17α-dimethyl-17β-hydroxy-5α-androst-2-ene or
2,17a-dimethyl-17b-hydroxy-5a-androst-2-ene
Read the full profile here.
Methoxygonadiene (M-LMG)
Structure:
http://www.totalflexblog.com/wp-cont...ygonadiene.png
Nomenclature:
18-methyl-3-methoxy-estra-2,5(10)-dien-17-one or
13β-ethyl-3-methoxy-gona-2,5(10)-dien-17-one
Synonyms:
Methoxygonadiene, methoxydienone, Max-LMG, M-LMG
Anabolic:Androgenic Ratio:
Unknown
History:
Methoxygonadiene is a chemical intermediate in the synthesis of steroids such as Norbolethone, 18-methyl-nortestosterone, and Norgestrel/Levonorgestrel.
Anabolic and Androgenic Activity:
Methoxygonadiene is believed to act as a "prodrug" to the biologically active steroid 18-methyl-19-nortestosterone.
Read the full profile at the Total Flex Blog.
Structure:
http://www.totalflexblog.com/wp-cont...imethazine.png
Nomenclature:
2a,17a-dimethyl-5a-androstan-17b-ol-3,3′-azine, or
2a,17a-dimethyl-5a-androstan-17b-ol-3-one-azine
Synonyms:
Dimethazine, dymethazine, Roxilon, mebolazine
Anabolic:Androgenic Ratio:
210:95-97
Read the full profile here.
Structure:
http://www.totalflexblog.com/wp-cont...stosterone.jpg
Nomenclature:
17β-hydroxy-4-androstene-3,11-dione
Synonyms:
11-Spray, Icon, XI-KT
Anabolic:Androgenic Ratio:
Unknown
History:
11-ketotestosterone was first released as an oral product called Icon by StarChem Labs in 2008. It was subsequently sold as the active ingredient in 11-KT spray, a topical product by Prototype Nutrition, in 2010. In October 2013 Iron Legion released another topical 11-ketotestosterone product called XI-KT.
Structure and Function:
11-ketotestosterone is a naturally-occurring anabolic compound found in trace amounts in humans (it’s a metabolite of adrenal hormones). 11-ketotestosterone is the primary androgen in fish. 11-ketotestosterone is also a strong and selective inhibitor of the cortisol-activating enzyme 11β-HSD1.
Read the full profile here.