jcem.endojournals.org/cgi/conten … 84/10/3459
“Thus, we envision that an ideal SARM for the treatment of primary or secondary male hypogonadism (Table 1Go) would have the following profile: orally active, ideally with a pharmacokinetic profile consistent with once a day administration, capable of stimulating prostate, seminal vesicles, and other sex accessory tissues at doses equipotent to those needed to provide increases in muscle mass and strength and fat-free mass, support bone growth, and maintain/restore libido, virilization, and male habitus. Unlike testosterone which, when converted to DHT in the prostate has an enhanced proliferative activity in relation to other peripheral tissues, these SARMs are not substrates for 5{alpha}-reductase activity, nor do they affect the activity of the enzyme.”
So apparently a “Selective Androgen Receptor Modulator” is in the works that has all the benefits of testosterone therapy without having potentially ill-effects on the prostate. That is, it’s a “partial agonist” in the prostate, and so reduces androgen stimulation there.
But what I’m really wondering about this drug, is whether such partial inhibition might occur in the androgen receptors of the hypothalamus, in a way similar to that of SERMS which act as partial inhibitors of hypothalamic estrogen receptors.
It would then act to enhance GnRH release, perhaps stimulating the HPTA in a “therapeutic” manner (as SERMS apparently are able to do), while at the same time acting as a T agonist.
Basically, I’m wondering whether this could play a role in “repairing” the HPTA, in a way similar to its SERM counterpart.
On the surface, at least, it seems that a combination of T and E partial agonists (SERMS and SARMS), acting upon the hypothalamus, and giving the hypothalamus the illusion of “low T” and “low E” might go far in stimulating the mechanisms opposite those operating under the fin-induced “high T” “high E” mileau, and maybe even “healing” the hypothalamus by this mechanism.
It’s a simple, unelaborated approach, but makes sense in my mind, if only in an Occam’s Razor, “turn the key the other way,” kind of way.