Steroids Source Talk | Anabolic Steroid Forum - View Single Post - Masteron as an Anti-Estrogen

Armstrong · #1 (**permalink**) 11-07-2015, 06:19 AM

Masteron as an Anti-Estrogen

I know it must seem like I sit around all day trying to find new uses for old drugs, but in this case, nothing could be further than the truth. Before I get into how and why you can use Masteron as an Anti-Estrogen, I’ll tell you a bit about where this idea came from, and why I’m telling you about it. And yes, this works in real life, not just on paper – I’ve used it and seen it used for this purpose successfully by several athletes.

A few years ago, I wrote my first piece on Masteron (Drostanolone Propionate), and discovered what its clinical use actually was: Reduction of breast cancer tumors, and as hormonal treatment of breast cancer. Well…the long version of that is that Masteron is an androgenic, anabolic steroid, used as an agent used to prevent or inhibit the growth of cancerous tumors.

Then, in one of those weird “duh” moments, I realized that gynocomastia, mastectomy, and Masteron all had that similar word root. You’d think that having an English degree would have helped me notice this fact sooner…anyway, I wrote the profile and didn’t think much about it anymore. I was then contacted by the owner of an underground lab, and asked why Masteron was always produced with a propionate ester, and whether it would be ok with a longer ester. This began another long period of research for me into Masteron. Well, I found out that Masteron would be fine with a longer ester, but I actually had a chance to test it out with that particular ester before it hit the market…I was still standing after 3 weeks on it, so it was produced en masse (as a side note that particular Underground Lab still produces it and it’s one of their better selling products).

So here I was with all of this research on Masteron and nothing to do with it. Well, after I took another look at the compound, a couple of things struck me. The first that struck me is that Masteron is made for women! Yeah…go back and read that again if you have to. Masteron is one of the few steroids that were actually created with women in mind, not men, and it’s the one that most people tell women to avoid! And the other thing that I noticed right away was that it is used for treatment of breast cancer. In particular, it’s used for the treatment of estrogen dependant breast tumors. By now, I’m sure you see where I’m going with this…Nolvadex is used clinically for this same purpose, as is Arimidex, Femera, Aromasin (a steroidal Aromatase Inhibitor), and Teslac (a steroid, technically). That’s some good company to be in, if you’re a steroid. But interestingly, Teslac is actually a steroid also, and Aromasin is a Steroidal Aromatase Inhibitor. So why can’t a “real” steroid do the same job at preventing breast cancer? Well, the answer is that it can!

To understand why Masteron can be used as an anti-estrogen, first we need to know that it’s derived from DHT. Why is this important?

This is important because DHT directly inhibits estrogenic activity on tissues. It is possible that it does this, possibly by acting as a competitive antagonist to the estrogen receptor or by decreasing estrogen receptor binding. Either way, it has multiple hypothesized mechanisms of action in some tissues. It has also been hypothesized that DHT actually suppresses estrogen’s effects not by inhibition of synthesis of estrogen receptor, but by (get ready…big words coming up) decreasing estrogen-induced RNA transcription at some point after the actual estrogen receptor binding has occurred. This means, in much simpler terms, that the estrogen gets to the receptor, but just doesn’t do its job (1). This means you can take steroids that convert to estrogen (called aromatizable steroids) and not worry about that estrogen possibly making you retain water, gain fat, or watch “Desperate Housewives.” Also, this could mean that the antiestrogenic effect of DHT is mediated by an androgen receptormediated mechanism. In fact, DHT has been shown to prevent the estrogen-dependent augmentation of the progesterone receptor in human breast cancer cells. And, not to be redundant, but it’s important to remember that virtually all of the anti-estrogens we use to control gyno and water retention are also used to treat breast cancer. So, now we know have observed that androgens are capable of inhibiting both the estrogenicinduction and the ongoing stimulation of PRc synthesis, but have no apparent effect upon basal concentrations of this receptor. Dihydrotestosterone (DHT) demonstrates a very high degree of inhibition of estrogen in human breast cancer cells. (2). But it’s not just DHT that does this; its metabolites have been shown to inhibit aromatization itself; DHT, androsterone, and 5alpha-androstandione are all potent inhibitors of the formation of estrone from androstenedione. In fact, it’s so potent at reducing estrogen that transdermal DHT gel applied to the affected area has been used to treat gynocomastia (3). DHT is such a potent anti-estrogen that it been even been used to increase height in children with short stature, and since it’s been determined that this increase is not due to GH-mediated effects, it was strongly suggested that DHT’s anti-estrogenic effects are the mechanism by which it can increase height (4) Of course, I suspect I don’t need to tell you that DHT is structurally incapable or converting to estrogen…

So all of this tells us that DHT will certainly have beneficial effects on keeping our estrogen in check, but what about Masteron? Can it be used as effectively? Well, let’s take a look at what Masteron actually is, relative to DHT. But before we can do that, I think a quick explanation of DHT is in order first. Don’t worry; I’ll make it as brief and painless as possible.

DHT is actually the result of testosterone interacting with the 5alpha-reductase (5a-R) enzyme. This enzyme is present in the scalp, prostate, external genitalia, and other places. As far as I can see, it apparently exists for the sole purpose of converting a steroid with a double bond between carbon 4 and carbon 5 to one with a single bond between them, and subsequently adding a hydrogen atom to each carbon. This process is called (of course) 5alpha-reduction.

So now we know how testosterone becomes Dihydrotestosterone. And everything would be great if this is the only thing that happened to our good old friend testosterone, because as you may already know, DHT is a far more potent androgen than testosterone. But, unfortunately, this is not the end of the story, because DHT is largely deactivated by the enzyme 3-alpha Hydroxysteroid Dehydrogenase (3bHSD), which is mainly present in skeletal muscle.

For our purposes here, we’re only going to be concerned with one particular action of this enzyme. It can either converts a steroid with a keto group on position 3 of the steroid to one with a hydroxy group in that position, thus converting DHT is to androstanediol. This conversion is part of reason DHT alone has not proven to be a very effective muscle builder, as androstanediol is not going to be very anabolic at all. If you look off to the left of the following molecular diagram, and compare it to the one above for DHT, you’ll notice that the “O” (oxygen) has been replaced with an “HO” (hydrogen + oxygen) at the third position: