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  1. #21
    Super Moderator Feedback Score 2 (100%) h2s's Avatar
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    Trenavar

    em5jb.jpg

    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].

    2licwab.jpg

    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.

  2. #22
    Super Moderator Feedback Score 2 (100%) h2s's Avatar
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    Mentabolan

    18opsj.jpg

    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

  3. #23
    Super Moderator Feedback Score 2 (100%) h2s's Avatar
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    Methyldiazirinol

    Structural Image:


    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.

  4. #24
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    Dimethandrostenol

    Structural Image:


    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.

  5. #25
    Super Moderator Feedback Score 2 (100%) h2s's Avatar
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    Methoxygonadiene (M-LMG)

    Structure:


    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.

  6. #26
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    Dimethazine

    Structure:



    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

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  7. #27
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    11-Ketotestosterone

    Structure:


    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.

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