Syntrax chemist gets credit
Syntrax did the same thing with penabol extreme except for they are using 5-androstendiol ether. They were the first ones to come up with the idea. If you read this article by Syntrax he indicates that other versions would work quite well. I tried penabol extreme for several weeks but saw no results, however as Syntrax indicates the other versions would be like legal drugs. Like Pat Arnold, Derek W.Cornelius chemist and owner of syntrax is constantly being ripped off by copycats, but hey it sounds much better then his version, kinda like 1-test being better then 1AD.
Several weeks ago, we looked closely at the present situation with taking steroidal
compounds orally. Up until now you had basically two choices. One was to go the
dietary supplement route and take compounds which had an extremely low oral
bioavailability. The other was to go the pharmaceutical route and take steroids that
alkylated at the 17a position of the steroid.
The first way works ok but you have to take large dosages throughout the day which is neither convenient nor economical. The second way works very well but has the
potential to damage your liver. Dilemma, dilemma!!!!
We saw a few weeks ago an entirely new technology that was presented to us by a
leader in the dietary supplement industry. We have been working on this technology for over one and a half years perfecting it. For the most part, it will work with any androgen/anabolic steroid. Here lies the problem!
Some snakes in this industry want to release nandrolone and testosterone 17 ethers
which are orally active. These are very good ideas for pharmaceuticals but for dietary supplements they are about the worst idea I have ever heard. Unfortunately, it shows no ingenuity and no concern for this industry. In this industry though, it is par for the course. Companies abound that only want to make a quick buck, lie about their products and rip off the consumer.
If you see or hear of any company that is selling or planning on selling these
compounds, then please, please call or write them and tell them ABSOLUTELY to stop.
For the sake of the industry, we do not need obvious drugs being pawned off as
supplements. They will work fairly well I predict if the dosage is high enough but it
could be one of the worst possible things for this industry.
As I promised in my last article, I will explain fully today how these steroidal ethers or
prosteroids work. Some so-called “experts” are trying to say that these compounds are resistant to enzymes or some other nonsense. This just shows the lack of knowledge these people have and proves the fact that they heard about this idea from us and rushed to tell everyone about it.
Where can we find the key that unlocks the secret doors to these prosteroids. Some may try to find them in the literature that deals with Quinbolone. But, behold you will quickly find that the authors knew only that the technology worked. To their chagrin, they did not understand the mechanisms behind this awesome technology.
The answer to our questions lies fully in a compound called Mepitiostane. This
compound was developed as an oral alternative to the powerful anabolic steroid
Epitiostanol.
What the…? I realize that most of you have never heard of Epitiostanol as it is a
relatively obscure steroid used for breast cancer that is only available in Japan. Again you might say, “How does a drug used for breast cancer work for us extreme fitness types?” Well, Epitiostanol was actually developed back in the 1960’s and has an
extremely good anabolic/androgenic ratio. This means that it causes a whole host of
positive effects in the body with minimal negative androgenic effects. The reason it was used for breast cancer is that it was shown to exert a potent anti-estrogenic effect which halted the progression of estrogen-stimulated cancers. What wonderful characteristics to have in a steroid! Great muscle growth with small androgenic phenomenon with no estrogenic problems like gyno…sounds like the perfect steroid!
Well, the Japanese company Shionogi thought so too but they wanted a characteristic
that epitiostanol lacked—significant oral bioavailability. The smart people at this
company went back into the literature and found that 17B steroidal ethers caused a
significant increase in oral bioavailability. They used the ether technology and voila,
they created Mepitiostane. Fortunately, they didn’t stop there! They decided to
elucidate just how these ethers work. Read below for the story!
The Shionogi research team began their quest by asking the question as to what
possible ways could the ether group be increasing bioavailability. They realized that
orally administered drugs and nutrients are transferred to the systemic circulation via the portal and/or lymphatic route following passage through the mucosal cell of the
intestinal lumen. They also understood that the portal route is considered to be the main route for compounds absorbed from the intestines because blood flow is about 500 times greater than lymph flow in capillaries of the villus.
Thus they first looked at the portal route and asked whether the ether group on the
steroid could be preventing the steroid from being metabolized by the liver. They looked at the characteristics of the molecule and decided that this was probably not the right answer.
Although not the primary place of absorption of most compounds, the intestinal
lymphatic system is known to play an important role in the absorption of some
compounds such as long chain fatty acids, triglycerides and lipid soluble vitamins. A
compound absorbed via intestinal lymphatics directly enters the systemic circulation at the level of the subclavian vein which avoids first pass metabolism of the compound
through the liver.
With this in mind, our good friends at Shionogi decided to look here for their answers.
Hey, all I can say is that these guys were right on the money! Using radioactive labeling of both Epitiostanol and Mepitiostane, they found that Epitiostanol is almost entirely absorbed via the portal route while mepitiostane is almost entirely absorbed via the lymphatic route. Bingo!
One of the most fascinating things that I noticed in their research was that there are
literally a multitude of factors that determine the bioavailability of orally consumed
steroids. Intestinal absorption usually refers to the process of uptake of a compound
from the site of absorption into the systemic circulation. This process includes the
penetration through the epithelial cells, metabolism in the epithelial cells and transfer
from the epithelial cells into the portal vein or lymphatics. Any or all of these processes can significantly cause inhibition of absorption of the parent compound. I have heard for quite some time from various sources that methandrostenolone (Dianabol) works much better when taken orally than injected. I used to scoff at this but now I might be in a position to believe what I heard. You see, there is quite a bit of research which shows that anabolic steroids undergo significant metabolism in the epithelial cells. Consequently, ingested methandrostenolone, as well as other orally administered steroids, could possibly be significantly converted into other active species with highly different characteristics before it even reaches the liver!
In the magazines and advertisements, we hear all the time that taking so and so amount of prohormone will give you thus and thus blood levels of that particular steroid. They base this simply by saying that a certain predefined percentage makes it through unmetabolized by the liver. They do not consider the facts that a great amount might not get absorbed by the epithelial cells nor do they take into consideration the fact that much might get metabolized into either more or less active species. Basically, the whole situation is quite complex and cannot be simplified with such a sophomoric formula.
I also want to bring up the point again of how important it is to have a proper delivery
system to cause increased penetration/absorption in the epithelial cells. I dug up a
bunch of research which shows that without any type of delivery system as much as
50% of the ingested steroid can be unabsorbed. You can guess what happens to this
unabsorbed steroid! Into the toilet my friend; into the toilet!!!
After Shionogi showed that steroidal ethers are absorbed in the lymphatic system, they did a series of studies which determined exactly what was responsible for lymphatic versus portal partitioning. Please understand that when the steroid is absorbed into the epithelial cell it is PARTITIONED or directed into either the portal vein or the lymphatic system. I already know what you are asking, “What determines the partitioning?”
It is a phenomenon called SUPERLIPOPHILICITY! If you remember correctly fatty acids and triglycerides are almost completely absorbed into the lymph. Superlipophilicity makes the compound associate so strongly with triglycerides and fatty acids that it absorbs in a similar fashion. During absorption, superlipophilic compounds become incorporated into the core lipids of chylomicrons in the intestinal mucosal cells of the intestinal mucosa. These fatty chylomicrons are then transferred almost exclusively into the lymphatic system (including the steroidal ethers).
We have to be careful here in assuming that all steroidal ethers are superlipophilic. My staff and I and have been doing very specific tests on these compounds to ensure that the steroidal ether we commercially market is superlipophilic in nature. Some companies will inevitably arbitrarily market a steroidal ether in hopes that it will work well—I just hope that their customers are not terribly disappointed. In our lab, we have seen very good and very bad steroidal ethers. It is really a very exact science!
We will soon be developing the very best steroidal ethers on the market—guaranteed to be superlipophilic! Furthermore, they will designed to have a very high
absorption/penetration into the epithelial cells. Of course, there is little we can do about the compounds being metabolized in the epithelial cells but from our initial experiments, I can guarantee you that this won’t matter!
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