I don’t think I understand this, mainly because I don’t understand 5ar conversion.
Could you (or someone else) please explain? Is there a way to know whether one is an efficient 5ar converter or not?
Regarding 5α-reductase (5AR) conversion:
Testosterone Metabolism
After testicular secretion, a small proportion of testosterone undergoes activation to two bioactive metabolites, estradiol and DHT, whereas the bulk of secreted testosterone undergoes inactivation by hepatic phase I and II metabolism to inactive oxidized and conjugated metabolites for urinary and/or biliary excretion (108).
The amplification pathway converts ~4% of circulating testosterone to the more potent, pure androgen, DHT (50, 52). DHT has higher binding affinity to (109) and 3-10 time greater molar potency in transactivation (110-112) of the androgen receptor relative to testosterone.
Testosterone is converted to the most potent natural androgen DHT by the 5a-reductase enzyme that originates from two distinct genes (I and II) (113). Type 1 5a-reductase is expressed in the liver, kidney, skin, and brain, whereas type 2 5a-reductase is characteristically expressed strongly in the prostate but also at lower levels in the skin (hair follicles) and liver (113).
DHT circulates at ~10% of blood testosterone concentrations, due to spillover from the prostate (122-123) and nonprostatic sources (124).
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Dihydrotestosterone has anti-estrogenic properties as it competes with other substrates for binding to the aromatase enzyme.
Mesterolone is a modified form of dihydrotestosterone and is believed to have anti-estrogenic properties.
William Llewellyn's ANABOLICS
Andractim® (dihydrotestosterone)
Description: Andractim is a prescription steroid preparation that contains the potent androgenic steroid dihydrotestosterone. This product comes in the form of a transdermal gel, typically containing 2.5% dihydrotestosterone by weight in an 80 gram tube. As with Androgel, roughly 10% of the active steroid will make it into circulation with each application.This would equate to 80 doses of 25 mg, with each dose delivering approximately 2.5 mg of steroid to the body.
Dihydrotestosterone itself is the most active androgen in the human body, displaying an ability to bind and activate the androgen receptor at least three or four times greater than that of its parent steroid testosterone. This trait, however, is not accompanied by equally powerful anabolic tendencies. In the case of dihydrotestosterone, we have a steroid that is almost purely androgenic, with only minimal muscle-building (anabolic)action.
Dihydrotestosterone is a weak muscle builder because it is extremely open to alteration by the 3-alpha-hydroxysteroid-dehydrogenase enzyme, responsible for breaking down active steroids like DHT into their inactive metabolites. 3a-HSD is present in high quantities in muscle tissue, running interference between the outer cell membrane and the androgen receptors that all steroid hormones are trying to reach. In humans, little DHT ends up actually reaching this receptor. Testosterone is very resistant to this enzyme, however, which allows it to be a much more effective muscle-building agent. 3a-HSD steroid deactivation in muscle tissue causes the same problem with Proviron (1-methyl-dihydrotestosterone).
DHT and Proviron both have very effective uses in areas such as fat loss, hardening, increasing CNS activity,and pure strength gains, but they do not perform well as anabolic agents.
Dihydrotestosterone is not aromatized by the body, and is not measurably estrogenic. An anti-estrogen is not necessary when using this steroid, as gynecomastia and water retention should not be concerns even among sensitive individuals.
DHT also has inherent anti- estrogenic properties, competing with other substrates for binding to the aromatase enzyme. Percutaneous dihydrotestosterone may be an effective option for the treatment of gynecomastia. Studies have reported a good level of success when treating certain forms of this disorder with Andractim, the drug affecting the ratio of androgenic to estrogenic action in the breast area enough that a notable regression of mammary tissue has been achieved in many cases.
Proviron (Mesterolone)
Mesterolone is actually believed to act as an anti-aromatase in the body, preventing or slowing the conversion of steroids into estrogen. The result is somewhat comparable to Arimidex®, although less profound. The anti-estrogenic properties of mesterolone are not unique, and a number of other steroids have demonstrated similar activity. Dihydrotestosterone and Masteron (2-methyl-dihydrotestosterone), for example, have been successfully used as therapies for gynecomastia and breast cancer due to their strong androgenic and potentially anti-estrogenic effect.
