3-Alpha

3-Alpha (5alpha-androstane-3alpha, 17beta-diol) contains the brand new 3-alpha isomer of 5alpha-androstanediol, a direct precursor to the extremely potent non-aromatizable (no estrogen) androgen dihydrotestosterone. It has a documented active blood conversion rate of 43%, a value four and a half times greater than the old 3-beta isomer. 3-Alpha is the ultimate body sculpting agent, excellent for enhancing muscle hardness, definition, strength and the overall look of solid muscularity.

U.S. Patent # 6,242,436

Just as there is a clear need for aromatizable anabolic steroid hormones, particularly when muscle mass is the primary focus, there also exists a strong need for non-aromatizable compounds: Androgens that do the specific job of hardening and tightening the physique. Just ask any serious bodybuilder where he would be without this class of steroid at contest time. The non-aromatizable androgen is often indispensable to building a winning show physique. Recently this class of agent has been explored in the supplement market, and 3-Alpha (5a-androstane-3a,17b-diol) represents the greatest achievement in this area of research as it is both a direct precursor to the most potent androgen found in humans (dihydrotestosterone) and by far the most active in terms of documented blood conversion rate. The chemical structures of both are:

3-Alpha (5a-androstane-3a,17b-diol)

Dihydrotestosterone (5a-androstane-3-one,17b-ol)

3-Alpha is unquestionably the most potent non-aromatizable androgenic prohormone ever developed, the ultimate hardening, cutting and strength promoting agent.

The Highest Documented Conversion Rate

3-Alpha is not only an incredibly potent product because it converts to the powerful androgen dihydrotestosterone, but also because it is activated with an affinity far exceeding any other prohormone. 4-androstenedione and 4-androstenediol for example have demonstrated a conversion rate to testosterone of roughly 5.5% and 16% respectively. The 3-beta isomer of 5-alpha androstanediol, the predecessor to 3-Alpha, stands at about a 9.5% conversion rate to dihydrotestosterone. Although these figures are fair, they fall far short of the 43% conversion rate demonstrated in in-vivo human studies with 3-alpha[i]. A blood conversion rate this high is clearly unprecedented, making 3-Alpha a serious step up from the less active prohormones to come before it. Figure 1 compares the active conversion rates of the mentioned compounds.

…43% conversion rate demonstrated in in-vivo
human studies with 3-alpha. A blood conversion
rate this high is clearly unprecedented…

Figure 1. 4-Androstenedione and 4-Androstenediol: The amount of testosterone formed after incubation in human blood. Acta Endocrinol vol. 55 697-704. 3-beta and 3-alpha isomers of 5alpha-androstanediol: The amount dihydrotestosterone formed in serum after injection into human subjects. Acta Endocrinol Vol. 79 (1975) 394-402.

No Aromatization

3-Alpha will not raise estrogen levels in the body, as it lacks the necessary structure for aromatization (androgen to estrogen conversion) to be possible. Its activity in the body is that of a pure androgen, and similarly side effects related to estrogen such as increased body fat, water retention and gynecomastia are not possible during use. Dihydrotestosterone is further shown to have anti-estrogenic activity, an added benefit when we are looking to lower the activity of this hormone in the body. Although some estrogen is desirous when we are looking to build mass, due to the fact that androgens and estrogens play opposing roles on the deposition of body fat in humans its absence is preferred when we are trying to “cut-up”. With this in mind bodybuilders will often use non-aromatizable steroids such as stanozolol, methenolone, trenbolone, fluoxymesterone, Proviron (mesterolone; 1-methyl DHT) and Masteron (drostanolone; 2-methyl DHT) exclusively during contest season. As a natural supplement of this type, 3-Alpha is the ultimate body-sculpting agent. Unmatched in its capacity to improve muscle hardness, definition and the overall look of solid muscularity often unattainable with estrogenic prohormones.

Anabolic Activity and Muscle Tissue Conversion

Dihydrotestosterone is not the best bulking agent for two reasons. First, it is non-estrogenic, and estrogenic activity seems to be an integral property of every good mass-building steroid. This is likely due to the interactions between estrogen and muscle glucose utilization[ii], growth hormone secretion[iii] and androgen receptor proliferation[iv]. So if bulk is the goal, then you probably do not want to use non-aromatizable prohormones exclusively. Dihydrotestosterone is also very open to the 3alpha-hydroxysteroid dehydrogenase enzyme, present in large amount in skeletal muscle tissue[v]. This works to rapidly deactivate DHT as it enters these cells by converting it to its metabolite (and precursor) 3-Alpha. This normally allows for poor androgen binding in muscle tissue, and a weak anabolic response. It would be incorrect to say that DHT was devoid of anabolic activity however, as it still exerts some activity in muscle. Interesting also is that fact that studies with 3-alpha note an unexpectedly high recovery of dihydrotestosterone in muscle tissue after administration. Although the 3A-HSD enzyme still appears to be preferential in its deactivation of DHT in this area of the body, we see a remarkable 23% conversion rate of 3-Alpha to dihydrotestosterone here. This is likely due to the fact that 3-Alpha relies on the same enzyme for activation that dihydrotestosterone does for deactivation, and as it enters muscle cells an opposite trend develops toward dihydrotestosterone buildup. Although not the preferred bulking agent, 3-Alpha does appear to have measurable anabolic potency, and is effective at promoting lean muscle tissue growth. Strength gains are also substantial, and especially profound in relation to overall bodyweight gain.

… [3-Alpha has] measurable anabolic potency,
and is effective at promoting lean muscle tissue
growth. Strength gains are also substantial, and
especially profound in relation to overall
bodyweight gain.

DHT and Androgenic Side Effects

It is a terrible misconception among bodybuilders that dihydrotestosterone is an isolated culprit when it comes to side effects. All anabolic/androgenic steroids exert their activities through the cellular androgen receptor, and dihydrotestosterone is no different than any other agent except that it is a more potent activator of this receptor than most. All steroids can cause androgenic side effects in direct relation to their affinity for this receptor, and DHT has no known unique ability in this regard. That said, those with a known or apparent genetic predisposition to hair loss for example would not be advised to take a strong androgenic prohormone if they wish to avoid advancing this condition. But again, 3-Alpha joins a long list of prohormones with similar potential (none are truly devoid of this possibility). For the vast number of others willing to experiment with prohormones, one would expect the typical androgenic side effects such as oily skin, acne or body and facial hair growth to occur with 3-Alpha in relation to the dosage used and ones own individual sensitivity.

A Naturally Occurring Hormone

3-Alpha (5-alpha androstane-3alpha,17beta-diol) is an androgen metabolite found in humans. It is similarly a natural compound that can legally be sold as a nutritional supplement.

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References:

[i] In vivo uptake and metabolism of 3b-5a-androstane-3a,17b-diol and of 3b-5a-androstane-3b,17b-diol by human prostatic hypertrophy. Horst, Dennis, Kaufmann and Voigt. Acta Endocrinol Vol. 79 (1975) 394-402

[ii] Aromatization of androgens to estrogens mediates increased activity of glucose 6-phosphate dehydrogenase in rat levator ani muscle. Endocrinol 106(2):440-43 1980

[iii] Activation of the somatotropic axis by testosterone in adult males: Evidence for the role of aromatization. Weissberger and Ho. J Clin Endocrinol Metab 76 (1993) 1407-12

[iv] Modulation of the cytosolic androgen receptor in striated muscle by sex steroids. Rance, Max. Endocrinol 115 (1984) 862-6

[v] In vivo androgen in rat skeletal and perineal muscles. Dionne, Dube, Lesage and Tremblay. Acta Endocr Copen. 91 (1979) 362-72