- Aromatase inhibitor, SHBG inhibitor, and estrogen-receptor antagonist.
- Ideal for PCT use, or as a standalone T-booster and performance enhancer.
D-Aspartic Acid is incredibly popular as a testosterone booster -- and for good reason, as studies have shown that a dose of 3000mg/day can dramatically increase testosterone levels in men. N-methyl D-Aspartate is simply a more powerful form of DAA: It appears to be 100 times more potent on an equimolar basis, and has a fundamentally-identical mechanism of action. Like DAA, it induces LH release and increases mRNA expression of the steroidogenic acute regulatory protein (StAR) -- a protein which shuttles cholesterol into the mitochondria of steroidogenic cells, and which represents the first rate-limiting step in steroid biosynthesis. There's no need to reference DAA studies: NMDA itself has been shown to dramatically increase testosterone in animal models.
MK-4 is the most active form of vitamin K, and is found in high concentrations in the testes. Studies in animals have shown that Vitamin K/MK4 deficiency leads to reduced expression of steroidogenic genes and low testosterone levels; another study has shown that MK-4 supplementation can increase testosterone levels via the induction of protein kinase A, CREB, and, most importantly, P450scc.
- PKA is a multi-functional enzyme which activates steroidogenic transcription factors such as steroidogenic factor 1, GATA-4, and the aforementioned StAR. Like StAR, PKA also directly facilitates cholesterol transport into the mitochondria of leydig cells. PKA is also a positive regulator of the P450scc enzyme.
- CREB is a upstream regulator of the aforementioned StAR, and increases in CREB expression have been shown to increase StAR promoter activity, StAR mRNA, and StAR protein levels in leydig cells.
- P450scc is the 'side-chain-cleavage' enzyme which converts cholesterol to pregnenolone -- and after StAR shuttles cholesterol into the mitochondria of steroidogenic cells, this becomes the rate-limiting step in testosterone biosynthesis. If StAR is sufficiently activated, P450scc is the bottleneck. Paragon amplifies P450scc expression with a hefty dose of MK-4 and destroys this bottleneck, allowing for much greater testosterone production.
Vitamin D represents another way to boost testosterone levels. Its mechanism of action has not been entirely elucidated, but seems to involve 17b-HSD induction. (ref, ref) While not a rate-limiting step, increases in 17b-HSD enzyme activity should increase the rate of conversion of DHEA to androstenediol, and therefore speed-up testosterone biosynthesis.
Regardless of mechanism, it's very clear that the stuff works: Vitamin D3 has been shown to increase testosterone levels in healthy adult males (ref), and two recent studies have shown a correlation between serum Vitamin D levels and testosterone levels. Vitamin D may also improve muscle function (ref, ref) and athletic performance. Given its many benefits, and its ability to potentially increase testosterone via a seemingly-unique mechanism, its role in Paragon is well warranted.
Forskolin is a potent cAMP-activator which should increase testosterone biosynthesis via a now-familiar mechanism: cAMP activation leads to Protein Kinase A phosphorylation and CREB induction, PKA and CREB both potentiate StAR, which then increases transport of cholesterol into the mitochondria. LH itself works in a nearly identical manner. At the dose contained in Prodigy It has been shown to increase testosterone levels in healthy adult men (ref). It also has beneficial effects where body composition is concerned -- due to increases in testosterone and induction of hormone sensitive lipase (HSL), an enzyme which is usually the rate-limiting step in lipolysis.
Euonymus Alatus and Prunella Vulgaris Extracts
Widely-used as Chinese herbal medicines, Euonymus Alatus and Prunella Vulgaris deliver a one-two punch to estrogen. Euonymous Alatus extract is a potent aromatase inhibitor with an IC50 of 11μm in Human placental aromatase. Animal studies have shown striking results: Treatment with EA extracts can lead to total estrogen deprivation in normal female rats. What's more, it displays selectivity for certain tissue types, and it may be much more selective and active towards aromatase enzymes expressed in breast tissue. This latter property may make it especially useful to people who are prone to gyno. It may be the most potent herbal aromatase inhibitor on the market today.
In contrast to Euonymus Alatus, Prunella Vulgaris interferes with estrogen receptor signalling indirectly. An unidentified compound within the extract binds to the aryl hydrocarbon receptor (AHR) as a full agonist, and this ligand-receptor complex seems to degrade the estrogen receptor protein via ubiquitin-mediated mechanisms. It seems to also compete with ER-mediated gene transcription via unknown mechanisms. One thing is certain: Estrogen is of no concern to anybody on Paragon!
Urtica Dioica extract It should be a shame to boost testosterone, only to have it deactivated by SHBG. Urtica Dioica (Stinging Nettle) root extract contains (-)-3,4-divanillyltetrahydrofuran and numerous other inhibitors of SHBG. We use a full-spectrum aqueous extract, which will help ensure that more of the testosterone you produce is put to good use.
PARAGON strongly targets every pathway to testosterone production, while still paying attention to estrogen, aromatase, and SHBG. There is no better PCT product on the market, and it's extremely potent as a standalone test-booster.
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