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Metribolone~methyltrienolone

heavyiron

Chemistry Experiment
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Metribolone (methyltrienolone)


Androgenic 6,000-7,000
Anabolic 12,000-30,000
Standard Methyltestosterone (oral)
Chemical Names 17alpha-methyl-17betahydroxyestra-4,9,11-triene-3-one 17alpha-methyl-trenbolone
Estrogenic Activity none
Progestational Activity no data available

Description:

Methyltrienolone is one of the strongest oral anabolic steroids ever produced. This agent is a derivative of trenbolone (trienolone), which has been c-17 alpha alkylated to allow for oral administration.This modification has created a steroid that is significantly stronger than its non-methylated cousin. Its potency has been measured to be anywhere from 120-300 times greater than that of methyltestosterone, with greater dissociation between anabolic and androgenic effects.625 626 Milligram for milligram methyltrienolone is a more active steroid than any agent sold on the commercial market, requiring doses as little as .5-1 milligram per day to notice a strong anabolic effect. Its potency is only matched by its relative toxicity, however, which has limited its modern use to that of laboratory research only.

History:

Methyltrienolone was first described in 1965.627 It was immediately identified as an extremely potent anabolic agent, far more potent than the commercially available agents of the time. In spite of its high relative activity, however, methyltrienolone has seen very limited use in humans. It was used clinically during the late 1960's and early '70's, most notably in the treatment of advanced breast cancer. Here, its exceedingly strong anabolic/androgenic action helps the drug counter the local effects of endogenous estrogens, lending it some efficacy for slowing or even regressing tumor growth. Such application was not long lived, however, as more realistic evaluations of the drug's toxicity soon led to its abandonment in human medicine.

By the mid-1970's, methyltrienolone was becoming an accepted standard in non-human research studies, particularly those pertaining to the study of the androgen receptor activity. For this purpose the agent is very well suited. Its sheer potency and resistance to serum-binding proteins makes it an excellent in-vitro receptor-binding standard to compare other agents to. Being so resistant to metabolism, active methyltrienolone metabolites are also not going to greatly interfere with the results of most experiments. Body tissues can metabolize most steroids fairly easily, which means that even incubation studies can be complicated with the question of what is causing a particular effect, the steroid or one of its unidentified metabolites. This is much less of an issue with methyltrienolone. Today, methyltrienolone remains an agent of research use only.

How Supplied:

Methyltrienolone is not available as a commercial agent.

Structural Characteristics:

Methyltrienolone is a modified form of nandrolone. It differs by: 1) the addition of a methyl group at carbon 17alpha to protect the hormone during oral administration and 2) the introduction of double bonds at carbons 9 and 11, which increases its binding affinity and slows its metabolism. The resulting steroid is significantly more potent than its nandrolone base, and displays a much longer half-life and lower affinity for serum-binding proteins in comparison. Methyltrienolone chemically differs from trenbolone only by the addition of a methyl group at c-17. This alteration changes the activity of methyltrienolone considerably, however, such that this agent should not simply be considered an oral form of trenbolone.

Administration (General):

Studies have shown that taking an oral anabolic steroid with food may decrease its bioavailability.630 This is caused by the fat-soluble nature of steroid hormones, which can allow some of the drug to dissolve with undigested dietary fat, reducing its absorption from the gastrointestinal tract. For maximum utilization, methyltrienolone should be taken on an empty stomach.

Administration (Men):

Methyltrienolone is no longer used in clinical medicine due to an unacceptable level of hepatotoxicity.This agent is generally not recommended for physique-or performance-enhancing purposes for the same reason. Those absolutely insisting on its use need to take its level of liver toxicity very seriously. At the very least, routine blood tests should be conducted to ensure the agent is not imparting damage. Drug duration should also be very limited, preferably to 4 weeks of use or less. The relative potency of methyltrienolone is extremely high, requiring doses as little as .5 milligram per day. Its effective and tolerable range is usually considered to be .5 to 2mg per day. Dianabol-type doses of 20-30 mg daily are completely unthinkable, and should never be attempted. Again, this is an extremely toxic steroid, and all good advice would say to avoid it. Anyone of the many commercially available steroids would be much safer choices.

Administration (Women):

Methyltrienolone is no longer used in clinical medicine due to an unacceptable level of hepatotoxicity.This agent is not recommended for women for physique-or performance-enhancing purposes due to its extremely strong toxicity and tendency to produce virilizing side effects.



Reference:
Llewellyn???s W. (2009). Anabolics (9th ed), Metribolone methyltrienolone(pp. 305-307): Jupiter, FL: Molecular Nutrition
 
over a hundred times stronger than methyltest and the highest anabolic ratio? So what's the deal? Does the toxicity destroy any gains? IS it pregame only? Liver cleanse after every dose?
 
Methyltrienolone (MT) is a very potent, reasonably toxic, non-aromatizing steroid. Ok. Lets go over those three points again. First of all, MT is potent. It binds so strongly to the AR (androgen receptor) that it is often used in studies on other androgens to measure how strongly they bind. In other words, this stuff binds onto the AR receptor so strongly that it is pretty much the benchmark for that quality. If youve read my profile on Trenbolone Acetate (TA), youll note that I said TA is the most potent injectable weapon in our arsenal with regards to ability to bind to the Androgen receptor. Thats still true, because this particular compound is not in our arsenal, and its not injectable... its simply the oral version of TA (i.e. it is Trenbolone which has undergone modification to become orally active, via the addition of a 17-alph-methyl group). So why is it important that this stuff binds so tightly to the AR? Well, Androgen Receptors are found in both fat cells as well as muscle cells(8); they act on the AR in muscle cells to promote growth, and in the fat cells to affect fat burning.(9)(6) The stronger the androgen binds to the A.R, the higher the lipolytic (fat burning) effect on adipose (fat)tissue(9)(5). Unfortunately, that strong binding doesnt also automatically mean that it will elicit the strongest possible anabolic response, nor that the weakest bind will elicit a weak anabolic response. Anadrol (oxymetholone) has the weakest bind to the AR possible (too low to be measured), and it produces a profound anabolic response, for example. Dianabol is simarly low, and produces a very good anabolic response. ARs are found in both muscle tissue as well as adipose tissue. When a muscles AR is stimulated, it can induce hypertrophy. When an adipose tissues AR is stimulated, through various related mechanisms, fat is lost. This is a gross oversimplification. Whatever. All we need to know is that when you have a steroid that binds to the AR, it builds muscle and burns fat. And a steroid that binds very tightly to the AR will stimulate a lot of muscle synthesis and burn a lot of fat. A good example of this is Trenbolone. And since I mentioned Trenbolone, its worth further mentioning that MT is basically a 17aa (oral) version of (injectable) Trenbolone. AR binding and AR stimulation is not the only mechanism which stimulates anabolism, however. It is important to note that dbol has a very low AR binding ability and A50 has an AR binding ability which is too low to even measure! Both are very potent oral steroids, though. So while its important, AR binding/stimulation is not the end all & be all of anabolism, although it is an important part. Dont be fooled by the anabolic/androgenic ratio of this (or any steroid), either. The anabolic/androgenic ratio of MT would suggest that it produces 120(+)x the anabolic and 60(+)x androgenic effect of Testosterone (which has a score of 100 and 100 respectively). If one were able to get a bottle of this stuff, I believe it would be best used as part of a cutting cycle, stacked with some injectables (testosterone, etc... ), but certainly no other orals. Its just too toxic. Negma (the French company who brought Parabolan to the market, and then discontinued it) never pushed MT to gain approval as a commercially released item, since their original studies showed it to be highly toxic. Methyltrienolone is, of course, a 19Nor compound (as is Trenbolone)...Thus, it will effect your sexual drive and performance in a similar way to both Tren and Nandrolone, meaning that Temporary Impotence and/or a lack of libido is highly possible (aka Tren-Dick or Deca Dick)(10). Another problem with MT is that it is a progestin, and binds shockingly well to the progesterone receptor also (PgR) (3). As we know, progestins amplify estrogenic effects of Aromatizing drugs. Although MT doesnt aromatize, you will still need to worry about its ability to cause side-effects by amplifying the estrogenic issues caused by the other compounds you may be taking. How toxic is this stuff? Well, it was never commercially marketed for use in humans, and has been relegated to Steroid-Purgatory, to be used only in studies. Id probably rate it on around the same level as taking very high doses of halotestin or methyltestosterone. And Id probably recommend that people keep doses of this product very low, much lower than recommended doses typical of the other 2 compounds I just mentioned (i.e. 500-750mcgs/day, for not much longer than 3-4 weeks). I have had the good fortune to discuss this product with the owner of an Underground Lab, and he had given out several samples of this stuff to athletes he knew, and they all kept records and got regular bloodwork done. People who were in the 2mg/day range developed highly elevated liver enzymes and Jaundice (yellowing of the eyes and skin). They all recovered, and through trial and error, a 500-750mcg dose was found to be (*relatively) safe, and (*roughly) as effective as 150-225mgs of Trenbolone Acetate. For women, a possible side effect of MT is Virilization (development of male sexual characteristics), which is profound with this stuff (11), so it is entirely off limits for women to use. You may want to take milk thistle with this compound, should you decide to try it, as well as (320mgs/day), ALA (500mgs per meal) and try some Pygeum Africanum (Permixon, the liposterolic extract of Serenoa)... stuff will all protect either your prostate or liver... in one study, it inhibited competitively the binding of Methyltrienolone to the cytosolic receptor of the rat prostate. Youll still need to get blood work done, avoid other orals (this includes drinking, or anything else which could tax your liver), and monitor your health closely. This isnt a drug for novices, clearly, and is probably only useful for pre-contest bodybuilders. Ive only seen MT available from one Underground Lab, and it came in a 50ml bottle, which was 1mg/ml, and was priced at $100. This translates to roughly 100 doses, at a reasonable cost of fifty-cents per dose. And since you would never want to run this particular drug for longer than 3-4 weeks at a time (maybe it would have use in the last few weeks before a bodybuilding competition, but not much else), youll get to use one bottle in 4 different cycles. That makes it no less dangerous, just reasonably cheap. Methyltrienolone Profile

[17beta-Hydroxy-17-methylestra-4,9,11-trien-3-one]
Molecular Weight: 284.3974
Formula: C19H24O2
Melting Point: N/A
Manufacturer: Negma (never released), Underground Labs
Effective dose: 500-750mcgs/day
Active Life: 4-6hours
Detection Time: Unknown (never tested in humans)
Anabolic/Androgenic Ratio (estimated):12,000+/6,000+
References:


  1. Endocrinology. 1984 Jun;114(6):2100-6.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.
  2. Bonne C, Raynaud JP. Methyltrienolone, a specific ligand for cellular androgen receptors. Steroids 1975 Aug;26(2):227-32
  3. Dube JY, Tremblay RR, Chapdelaine P. Binding of methyltrienolone to various androgen-dependent and androgen-responsive tissues in four animal species. Horm Res 1976;7(6):333-40
  4. Tremblay RR, Dube JY, Ho-Kim MA, Lesage R. Determination of rat muscles androgen-receptor complexes with methyltrienolone. Steroids 1977 Feb;29(2):185-95 5. APMIS. 2000 Dec;108(12):838-46.
  5. APMIS. 2000 Dec;108(12):838-46.
  6. (Xu X, et al. "The effects of androgens on the regulation of lipolysis in adipose precursor cells." Endocrinology 1990 Feb;126(2):1229 ).
  7. J Anim Sci. 1992 Nov;70(11):3381-90.
  8. Am J Physiol. 1998 Jun;274(6 Pt 1):C1645-52.
  9. Biochim Biophys Acta. 1995 May 11;1244(1):117-20.
  10. Baum MJ, Kingsbury PA, Erskine MS. Failure of the synthetic androgen 17 beta-hydroxy-17 alpha-methyl-estra-4,9,11-triene-3-one (methyltrienolone, R1881) to duplicate the activational effect of testosterone on mating in castrated male rats. J Endocrinol 1987 Apr;113(1):15-20
  11. Biochem Pharmacol. 1984 Apr 15;33(8):1235-41.Changes in the activities of microsomal enzymes involved in hepatic steroid metabolism in the rat after administration of androgenic, estrogenic, progestational, anabolic and catatoxic steroids.
 
MTR can be injected as well at a max inject dose of 3mg ED for 20 to 30 days MAX. Injecting removes it from first pass metabolism decreasing its toxicity.
 
Where can I find this??Very interested!!
 
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