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Saturday, July 18, 2009

Impatiently Waiting the Arrival of Iforce's PROTODROL!!

This morning I sat down, while drinking my protein and waximaize shake, with intentions of blasting the nutritional supplement industry for a lack of innovation and creativity. I planned on addressing that and the over abundance of copy-cat/clone supplements, but before I was able to type a word... My eyes were drawn to a beacon of light in the distance. This glorious beam of incandescence was set forth by none other than Iforce nutrition. So, for that Iforce, I salute you. Iforce has a decent line of hormonal and non-hormonal products. I believe they were one of the first companies to re-release 1,4-AD after the 2004 pro-hormone ban. They also have clones which I was hating on earlier, but I believe that is all part of a good hormonal selection which Iforce would like to provide. I say this because the last supp they came out with, Dimethazine, was a fairly innovative and exciting compound. Although I am not sure of the validity of the claims, Dimethazine was two Methasteron molecules bound by an azine bond which was claimed to slow release and decrease liver toxicity.
"Now what the hell is Chris talking about???" you ask. Well I am talking about the new supplement from Iforce Nutrition called Protodrol.

Ok let's get down to bidness, the claimed active ingredient within Protodrol is 17a-methyl-5a-androstan-17b-ol. First I'll break down the name... Right off the bat we see the 17a-methyl, ok it's 17-alpha alkylated for oral availability, from this we can expect good oral absorption with no need for conversion to another hormone via 17 beta-hydroxysteroid dehydrogenase. We can also expect liver toxcicity which is associated with all orally active hormones. However, Iforce claims a rare occurence with this oral which lowers its toxicity, but we will address this later. Next we notice the 5a-androstan, which means this is 5alpha-reduced and lacks the 4 to 5 carbon double bond. This will give us DHT like characteristics, considering DHT is the product of 5alpha-reductase and testosterone = 5a-reduced test. Next we see the expected 17b-ol which is the -OH @ the 17th position which will help us bind androgen receptors. Ok, all seems pretty common we have a methylated androstane... But, what about the third carbon? This is where we would usualy find a ketone, alcohol, or as we saw with Applied Nutraceuticals' The One in my previous post, a hydroxyimine. Well there is nothing. Nothing? Yes!! Nothing and here is the structure.
Generally speaking a 5alpha-reduced andro, causes the molecule to assume a chair confirmation which causes a flattening of the rings. This flattening is believed to increase androgenic activity. But, this molecule lacks an oxygen molecule @ the third position which is necessary for androgenic activity. It is believed that the androgenic activity of molecules lacking an oxygen at c-3 or c-17 is dependent upon the in-vivo oxygenation. I could not find any research on this molecule but according to Patrick Arnold of Ergopharm, this molecule has the same androgenic activity of methyl-testosterone and is 1.8 times more anabolic. In the write-up that Iforce released, a research article is quoted in saying steroids with saturated A-rings, such as in the case of Protodrol, do not induce increased levels of bilirubin. Bilirubin is a product of heme (a protein in red blood cells) catabolism. Bilirubin levels are evaluated for liver function tests. The rise in bilirubin can be associated with hepatoxic drugs. This does not necessarily mean it is not liver toxic, but it will be less stressful on one's body and liver.

So we have an oral with supposedly low toxicity, same androgenicity as methyl-test, and almost twice as anabolic! I love it, all we can do is wait and watch to see the real world results.

Thursday, July 2, 2009

E-911 to be released by LG Sciences

LG Sciences, formerly know as Legal Gear is releasing a stimulant based product, to accompany their product, T-911, in the sublingual department. T-911 is a blend of androsterone and some claimed test boosters/SERMS. All of these molecules are delivered sublingualy with cyclodextrin. Cyclodextrin is a cyclical carbohydrate compound composed of 5 or more, 6-8 membered, sugar rings.
According to LG's site E-911 is a blend of "Caffeine, Geranium Oil Extract(#105-41-9), Synephrine, and Hordinine" formed into a tasty little sublingual mint tablet. The first ingredient, caffeine, is not only expected but I believe it is required for an energy product in the supplement industry; so nothing worth discussing with this compound.
The second ingredient, Geranium Oil Extract, is also nothing new but somewhat more exciting than caffeine. Geranium Oil extract is used for the ingredient Geranamine AKA methylhexaneamine or 1,3-Dimethylamylamine, which is a potent stimulant. However, according to Jalali-Heravi M, Et al. 2006, " The major constituents in the Iranian geranium oil are beta-citronellol (47.46%), citronellyl formate (11.00%), geraniol (8.74%), iso-menthone (4.32%) and linalool (3.07%)." According to Ping Z Et al. 1996, Geranium oil contains only 0.66% Geranamine, so an extract of this oil would yield a bunch or chemicals one doesn't need or want and a little bit of Geranamine which is the desired compound. This would be resolved with a standardized extract, but LG does not list the extract as standardized. You bet your ass if it was standardized for a favorable percentage of geranamine this would be listed on the label. Sooo... it doesn't sound to good for you gernanamine stimulant junkies, does it? But, wait... calm your overly stimulated central nervous system down for one second. I don't believe LG copped out and started pushing weak ass geranium extract. The label lists the CAS registry number for... you guessed it, our prized geranamine. This leads me hypothesize that LG listed the ingredient as an extract to keep the FDA off of their back and pack there new sublingual stim with the powerful punch of synthetic geranamine.
Next on the list we have synephrine AKA Oxedrine, which is another common stimulant found in many fat loss formulations. There is not much info on oral administration of synepherine. The Dietary Supplement Label Database claims it is a "Sympathetic alpha-adrenergic agonist." However, according to Carpene C, Et al. 1999, Synephrine may act as a Beta-3 Adrenergenic receptor agonist. This type of beta agonist shows promising effects for weight loss through thermogenisis, increased metabolic rate, and increased insulin sensitivity, they have even shown beneficial to blood lipid profiles. (Clapham J, Et al. 2001) These effects sound excellent, but more research would be beneficial.

The final ingredient Hordenine, is a phenylalkylamine alkaloid, which is an indirectly acting adrenergic drug. LG claims that this will prolong and increase the effect of the stimulants in E-911 and prevent crashing. However, research claims that it promotes the release of Norepinepherine stores. (Wochenschr D, Et al. 1995) Now, considering Norepi or Noradrenaline has a stimulant effect itself, I don't see how Hordenine prolongs the effect of any stims. Norepi increases heart rate, triggers the release of glucose to the blood stream, and promotes blood flow to skeletal muscle. These can all be beneficial for athletic performance and physical appearance enhancement, but I do not see how it would directly increase and prolong the effect of the other ingredients.
Just as I was finishing up this post, I checked the LG website again and it seems they have added Lecithin, Chitosan, and Acacia Seed Extract into the mix. Lecithin, is used as a food binder or can be used as a coating for tablets, and I am assuming it is used for the latter. Chitosan, is used to bind fat and excrete it, to prevent absorption and metabolism, hence less caloric intake with meals. Although Chitosan is used and marketed for this purpose the efficacy is debated and not fully supported by scientific literature. Acacia catechu, is purported to have anti-oxidant properties, it also contains various psychoactive alkaloids such as DMT and 5-MeO-DMT in the leaf and bark. I can't really take a guess at what the Acacia extract was added for, or even which species of Acacia was used. For this reason I will keep my mouth shut.
Lg has produced a stimulant based tablet with the ability to dissolve under your tongue. This should deliver the ingredients fast and effectively with a big punch for you stim users and those trying to burn off the body fat. I don't know when this will be available but keep your eyes peeled for its release at your favorite supp store and reviews on the forums.